Read Members` reports Sept 2011

Transcription

Members‘ reports for the period 2011 - 2013
Questionnaire for ResNet NPND members’ report
1. Personal information
Schmidt
Name
Thomas J.
First name
Prof. Dr.
Academic title(s)
2. Affiliation – Institution, Department, Function
Institution: University of Münster
Department: Institute of Pharmaceutical Biology and Phytochemistry
Function: Professor
3. Report on activities in and for ResNet NPND since April 2011
Please give a short description on your activities within ResNet NPND (anything you did to advance joint
research with or among ResNet members, to promote the network).
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Organized the founding workshop of ResNet NPND in April 2011 at the University of Münster
and took the function of coordinator for Europe.
Organized joint Brazilian-German BMBF/CNPq proposal together with Alvaro Romanha (March
2011).
Established basic statutes for ResNet together with Brazilian coordinator A. Romanha (June
2011).
Established ResNet NPND website (June 2011).
Represented and introduced ResNet NPND at various meetings (ACMAP, Huntsville, USA (July
2011); Phytopharm 2011, Nürnberg, Germany (July 2011), DPhG/ÖPhG meeting, Innsbruck,
Austria (Sept. 2011); Symposium on neglected diseases, Sao Paulo, Brazil (Nov. 2011); COST CM
1801 meeting, Siena, Italy (June 2012); GA meeting New York, USA (Aug. 2012); COST CM 1801
meeting, Kolymvari, Greece (Sept. 2012); GA meeting, Münster, Germany (Sept. 2013);
NAPRECA meeting, Khartoum, Sudan (Dec. 2013).
Organized 2-part review in Current Medicinal Chemistry to which 16 members of ResNet NPND
contributed (published in 2012).
Guest editor of special issue “Natural products against neglected diseases” in “Molecules”
(2013/2014, ongoing).
Organized CAPES-WWU guest professorship for Fernando Ca Costa at the University of
Münster, Topic "In silico-tools to assess the bio-and chemodiversity of Natural Products with
respect to their potential as new lead compounds againts Neglected Diseases" and hosted Prof.
Da Costa from Sept. 2012 to April 2013.
Organized and held members’ meeting at GA2013 (Münster, Germany) and prepared report on
activities of ResNet NPND (distributed Oct. 2013).
Organized new members’ application and evaluation (Oct. 2013-Feb. 2014).
Organized and collected members’ reports for the period 2011-2013.
Established and/or continued direct cooperations with the following ResNet members:
o Reto Brun
o Fernando B. Da Costa
o Norberto P. Lopes
o André G. Tempone
o Marcus T. Scotti
o Gerold Jerz
o Sami A. Khalid (new member)
o Adeleke Adebajo (new member)
o Jong Seong Kang, Young Ho Kim (new members)
4. Publications relevant to the field
Please give full bibliography of all your scientific publications relevant to the field in the years 2011, 2012
and 2013. Please mark those that were co-authored by at least one further member of ResNet NPND in
red (irrespective of whether you made an acknowledgement to ResNet NPND, or not).
Schmidt, T.J., Kaiser, M., Brun, R. Complete structural assignment of Serratol, a cembrane type diterpene
from Boswellia serrata, and evaluation of its antiprotozoal activity. Planta Med. 77, 849-850 (2011).
Maas, M., Hensel, A., da Costa, F.B., Brun, R., Kaiser, M., Schmidt, T.J. An unusual dimeric guaianolide
with antiprotozoal activity and further sesquiterpene lactones from Eupatorium perfoliatum.
Phytochemistry 72, 635-644 (2011).
Harel, D., Khalid, S. A., Kaiser, M., Brun, R., Wünsch, B., Schmidt, T.J., Encecalol angelate, an unstable
chromene from Ageratum conyzoides L.: Total Synthesis and Investigation of its Antiprotozoal Activity. J.
Ethnopharmacol. 137, 620-625 (2011).
Gökbulut, A., Kaiser, M., Brun, R., Sarer, E., Schmidt, T.J. 9β-Hydroxyparthenolide esters from Inula
montbretiana DC. and their antiprotozoal activity. Planta Med. 78, 225-229 (2012).
Schmidt, T.J.; Khalid, S.A.; Romanha, A.J.; Alves, T.M.A.; Biavatti, M.W.; Brun, R.; Da Costa, F.B.; de
Castro, S.L.; Ferreira, V.F.; de Lacerda, M.V.G.; Lago, J.H.G.; Leon, L.L.; Lopes, N.P.; das Neves Amorim,
R.C.; Niehues, M.; Ogungbe, I.V.; Pohlit, A.M.; Scotti, M.T.; Setzer, W.N.; Soeiro, M. de N.C.; Steindel, M.;
Tempone, A.G. The potential of secondary metabolites from plants as drugs or leads against protozoan
neglected diseases – Part I. Current Med. Chem. 19, 2128-2175 (2012).
Schmidt, T.J.; Khalid, S.A.; Romanha, A.J.; Alves, T.M.A.; Biavatti, M.W.; Brun, R.; Da Costa, F.B.; de
Castro, S.L.; Ferreira, V.F.; de Lacerda, M.V.G.; Lago, J.H.G.; Leon, L.L.; Lopes, N.P.; das Neves Amorim,
R.C.; Niehues, M.; Ogungbe, I.V.; Pohlit, A.M.; Scotti, M.T.; Setzer, W.N.; Soeiro, M. de N.C.; Steindel, M.;
Tempone, A.G. The potential of secondary metabolites from plants as drugs or leads against protozoan
neglected diseases – Part II. Current Med. Chem. 19, 2176-2228 (2012).
Schmidt, T. J., Rzeppa, S., Kaiser, M., Brun, R. Larrea tridentata – Absolute configuration of its
epoxylignans and investigations on its antiprotozoal activity. Phytochem. Lett., 5 632–638 (2012).
Adebajo AC, Odediran SA, Nneji CM, Iwalewa EO, Rukunga GM, Aladesanmi AJ, Gathirwa JW, Ademowo
OG, Olugbade TA, Schmidt TJ, Verspohl EJ. Evaluation of Ethnomedical Claims II: Antimalarial Activities of
Gongronema latifolium Root and Stem. Journal of Herbs, Spices & Medicinal Plants, 19, 97–118 (2013)
Harel, D., Schepmann, D., Prinz, H., Brun, R., Schmidt, T.J., Wünsch B. Natural product derived
antiprotozoal agents: Synthesis, biological evaluation and structure-activity relationships of novel
chromene and chromane derivatives. J. Med. Chem. 56, 7442-7448 (2013).
Harel, D., Schepmann, D., Prinz, H., Brun, R., Schmidt, T.J., Wünsch B. Enantioselective synthesis of
encecaline-derived potent antimalarial agents. Org. Biomol. Chem. 11, 7342-7349 (2013).
Schmidt TJ, Da Costa FB, Lopes NP, Kaiser M, Brun R. In silico prediction and experimental evaluation of
furanoheliangolide sesquiterpene lactones as potent agents against Trypanosoma brucei rhodesiense.
Antimicrob. Agents Chemother. 58, 325-332 (2014).
5. Motivation to continue membership
Please give a short statement explaining why you wish to continue your membership and cooperation
with ResNet NPND.
Because I strongly believe in the success of this network if we continue to bundle our efforts towards a
common goal!
6. Evaluation of ResNet NPND activities, future perspectives and suggestions for improvement
Please give a short statement describing your experiences with ResNet NPND, outline how you would
imagine ResNet NPND in the future, including constructive suggestions for improvement.
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It is wonderful to cooperate with many people and coordinate the joint work (example: review
w./ 100 printed journal pages).
Difficulties to acquire “big money“ funds for a large network structure‐ consequence:
Funding obtained for smaller “sub‐nets“ can be combined in synergistic activities.
Difficulties in coordinating network without more feedback of (some) members; consequences:
o More stringent network structure is needed.
o Priority‐making and milestones to be defined more clearly.
o Clearer distribution of responsibilities is needed.
o Statutes and rules to be officially formulated and accepted (and followed) by members.
o More visibility is needed. Joint publications to be marked, internet presentation is to be
improved.
More cooperation between more than 2 network members is needed. The network still has too
many loose ends.
7. Confirmation of commitment, declaration of scientific independence and signature
I hereby confirm that I renew my commitment myself to the aims and goals of ResNet NPND and that I
wish to continue my membership in ResNet NPND.
At the same time I declare, that I am legally authorized to conduct own research projects, coordinate
joint research, publish data and work independently in a scientific environment.
I understand that I have the right to terminate my membership at any time, which in this case I must do
in written form, to a member of the executive board.
Münster
March 28, 2014
____________________________________________________________________
(Place)
(Date)
(Signature)
Please fill in, print and sign this form. It can be sent back as hardcopy or, preferably, as a scanned pdf
document to thomschm@uni-muenster.de
Questionnaire for ResNet NPND members’ report To all current members: Please fill in and send back by Oct. 15, 2013 1. Personal information Almeida Alves Name Tania Maria First name Dr Academic title(s) 2. Affiliation – Institution, Department, Function Institution: Centro de Pesquisas René Rachou CPqRR-‐ FIOCRUZ Department: Laboratorio de Química de Produtos Naturais (LQPN) Function: Researcher 3. Report on activities in and for ResNet NPND since April 2011 1) A collaborative project with Drs Gerold Jertz, Susana Leitão, Alvaro Romanha: Their PhD student Mariana Neves Vieira has been trained here, in CPqRR-‐FIOCRUZ for some bioassay. We are screening some plants extracts against Leishmania amazonensis and T. cruzi. 2) A collaborative project with Dr. Nazaré Soeiro: The Master student Luiza Castro from CPqRR-‐FIOCRUZ will be trained by Dr Soeiro at IOC-‐FIOCRUZ for run some bioassay aiming a investigation of possible mechanism of action of some leishmanicidal natural products. 3) The collaborative project with Dr Alvaro Romanha and Mario Steindel: Screening plant and fungi extracts against Chagas disease is kept. 4. Publications relevant to the field Please give full bibliography of all your scientific publications relevant to the field in the years 2011, 2012 and 2013. Please mark those that were co-‐authored by at least one further member of ResNet NPND in red (irrespective of whether you made an acknowledgement to ResNet NPND, or not). 1) FURBINO, L. E. ; GODINHO, V. M. ; Santiago, I. F. ; PELLIZARI, F. M. ; ALVES, T. M. A. ; Zani, C. L. ; SALES-‐JUNIOR, P A. S. ; ROMANHA, A. J. ; CARVALHO, A. G. O. ; GIL, L. H. V. G. ; ROSA, C.A. ; MINNIS, A . M. ; ROSA, L. H.. Diversity Patterns, Ecology and Biological Activities of Fungal Communities Associated with the Endemic Macroalgae Across the Antarctic Peninsula. Microbial Ecology, v. 67, p. 1, 2014. 2) GODINHO, V. M ; FURBINO, L. E ; SANTIAGO, I. F ; PELLIZZARI, F. M ; YOKOYA, N.S ; PUPO, D. ; ALVES, T. M. A. ; S JUNIOR, P. A ; ROMANHA, A. J ; ZANI, C. L ; CANTRELL, C. L ; ROSA, C.A. ; ROSA, L. H. Diversity and bioprospecting of fungal communities associated with endemic and cold-‐adapted macroalgae in A ntarctica. The ISME Journal, v. 7, p. 1434-‐1451, 2013. 3) T.J. SCHMIDT, ; S.A. KHALID ; ROMANHA, A. J. ; ALVES, T. M. A.; M.W. BIAVATTI ; F.B. DA COSTA ; S.L. DE CASTRO ; V.F. FERREIRA ; M.V.G. DE LACERDA ; J.H.G. LAGO ; L.L. LEON ; N.P. LOPES ; R.C. DAS NEVES AMORIM ; M. NIEHUES ; .V. OGUNGBE ; A.M. POHLIT ; M.T. SCOTTI ; W.N. SETZER ; M. DE N.C. SOEIRO ; M. STEINDEL ; A.G. TEMPONE . The Potential of Secondary Metabolites from Plants as Drugs or Leads Against Protozoan Neglected Diseases Part I. Current Medicinal Chemistry, v. 19, p. 2128-‐2175, 2012. 4) T.J. SCHMIDT, ; S.A. KHALID ; ROMANHA, A. J. ; ALVES, T. M. A. ; M.W. BIAVATTI ; R. BRUN ; F.B. DA COSTA ; S.L. DE CASTRO ; V.F. FERREIRA ; M.V.G. DE LACERDA ; J.H.G. LAGO ; L.L. LEON ; N.P. LOPES ; R.C. DAS NEVES A MORIM ; M. NIEHUES ; .V. OGUNGBE ; A.M. POHLIT ; M.T. SCOTTI ; W.N. SETZER ; M. DE N.C. SOEIRO ; M. STEINDEL ; A.G. TEMPONE . The Potential of Secondary Metabolites from Plants as Drugs or Leads Against Protozoan Neglected Diseases -‐ Part II. Current Medicinal Chemistry, v. 19, p. 2176-‐2228, 2012. 5) SANTIAGO, I. F. ; ALVES, T. M. A.; RABELLO, A. ; SALES JUNIOR, P. A. ;; ROMANHA, A.J. ; ZANI, C. L. ; ROSA, C.S A. ; ROSA, L. H. Leishmanicidal and antitumoral activities of endophytic fungi associated with the Antarctic angiosperms Deschampsia antarctica Desv. and Colobanthus quitensis (Kunth) Bartl.. Extremophiles (Tokyo. Print), v. 16, p. 95-‐103, 2012. 5. Motivation to continue membership Please give a short statement explaining why you wish to continue your membership and cooperation with ResNet NPND. I wish to continue my membership and cooperation with ResNet NPND because the network is formed by several expertise in areas that, together work better. This is an important tool to achieve the aim of fighting against world poverty. 6. Evaluation of ResNet NPND activities, future perspectives and suggestions for improvement Please give a short statement describing your experiences with ResNet NPND, outline how you would imagine ResNet NPND in the future, including constructive suggestions for improvement. The first meeting was crucial to establish new collaboration and cooperation. Challenges are: 1) Keep meeting and discussing, at least once each 2 years. Financial support is necessary for that. 2) One important feature is to homogenize the way bioassays are being running. The experience of Dr Brum would improve it a lot. 3) Training on dereplication process 4) Database where we could deposit and consult organisms and their natural products, bioactivity, physical, spectral and chromatographic data 7.
Confirmation
of commitment,
declaration of scientitic independence and signature
. I hereby confirm that I renew my commitment myself to the aims and goals of ResNet NPND and that I
_Belo Horizonte, March 7th, 2014
(Place)
(Date)
(Signature)
Please til! in, print and sign this formo It can be sent back as hardcopy or, preferably, as a scanned pdf
7.
Questionnaire for ResNet NPND members’ report To all current members: Please fill in and send back by Oct. 15, 2013 1. Personal information Da Costa Name Fernando B. First name Prof. Dr. Academic title(s) 2. Affiliation – Institution, Department, Function Institution: University of São Paulo, School of Pharmaceutical Sciences of Ribeirão Preto Department: Pharmaceutical S ciences Function: Associate Professor 3. Report on activities in and for ResNet NPND since April 2011 Please give a short description on your activities within ResNet NPND (anything you did to advance joint research with or among ResNet members, to promote the network). • Brazilian Ph.D. students at IPBP-‐WWU: M. Nogueira (plant metabolomics and bioassays, full Ph.D., since Feb. 2012, sponsored by CAPES) and T.B. Oliveira (in silico methods, sandwich Ph.D., since Oct. 2013, sponsored by FAPESP) • Guest professorship at IPBP-‐WWU (in silico methods and neglected diseases, 8 months, Sep. 2012 to Apr. 2013, sponsored by CAPES) • Invited lecture of Prof. T.J. Schmidt (to be held at CIFARP, Nov. 2013, Ribeirão Preto, Brazil, sponsored by FAPESP) • Participation in the ResNet NPND Members Meeting and in the ResNet NPND Workshop during the GA Meeting 2013, Münster, Germany (sponsored by FAPESP) • Poster Presentation during the GA Meeting 2013 (sponsored by FAPESP) • Joint publications with two ResNet NPND members (T.J. Schmidt and N.P. Lopes) 4. Publications relevant to the field Please give full bibliography of all your scientific publications relevant to the field in the years 2011, 2012 and 2013. Please mark those that were co-‐authored by at least one further member of ResNet NPND in red (irrespective of whether you made an acknowledgement to ResNet NPND, or not). Maas, M., Hensel, A., da Costa, F.B, Brun, R., Kaiser, M., Schmidt, T.J. An unusual dimeric guaianolide with antiprotozoal activity and further sesquiterpene lactones from Eupatorium perfoliatum. Phytochemistry 72, 635-‐644 (2011). Schmidt, T.J.; Khalid, S.A.; Romanha, A.J.; Alves, T.M.A.; Biavatti, M.W.; Brun, R.; Da Costa, F.B.; de Castro, S.L.; Ferreira, V.F.; de Lacerda, M.V.G.; Lago, J.H.G.; Leon, L.L.; Lopes, N.P.; das Neves A morim, R.C.; Niehues, M.; Ogungbe, I.V.; Pohlit, A.M.; Scotti, M.T.; Setzer, W.N.; Soeiro, M. de N.C.; Steindel, M.; Tempone, A.G. The potential of secondary metabolites from plants as drugs or leads against protozoan neglected diseases – Part I. Current Med. Chem. 19, 2128-‐2175 (2012). Schmidt, T.J.; Khalid, S.A.; Romanha, A.J.; Alves, T.M.A.; Biavatti, M.W.; Brun, R.; Da Costa, F.B.; de Castro, S.L.; Ferreira, V.F.; de Lacerda, M.V.G.; Lago, J.H.G.; Leon, L.L.; Lopes, N.P.; das Neves A morim, R.C.; Niehues, M.; Ogungbe, I.V.; Pohlit, A.M.; Scotti, M.T.; Setzer, W.N.; Soeiro, M. de N.C.; Steindel, M.; Tempone, A.G. The potential of secondary metabolites from plants as drugs or leads against protozoan neglected diseases – Part II. Current Med. Chem. 19, 2176-‐2228 (2012). Arakawa, N.S., Gobbo-‐Neto, L., Ambrosio, S.R., Ausech Antonucci, G. Vilela Sampaio, S. Tallarico Pupo, M., Said, S., Schmidt, T.J., Da Costa, F.B. Unusual biotransformation products of a sesquiterpene lactone by Aspergillus species. Phytochemistry, published online on 14 October 2013. Schmidt, T.J., Da Costa, F.B., Lopes, N.P., Kaiser, M., Brun, R. In silico prediction and experimental evaluation of furanoheliangolide sesquiterpene lactones as potent agents against Trypanosoma brucei rhodesiense. Under revision. 5. Motivation to continue membership Please give a short statement explaining why you wish to continue your membership and cooperation with ResNet NPND. I plan to cooperate with ResNet NPND as follows: • to write a scientific project application involving the screening of extracts of Brazilian Asteraceae against the enzyme dihydroorotate dehydrogenase (DHODH) from Plasmodium falciparum and Trypanosoma cruzi, including the use of in silico methods such as QSAR, docking, and virtual screening; • to supervise a Ph.D. project (to start 2014) involving part of the scientific project described above; • to collaborate with Prof. M.T. Scotti (UFPB, BR) in the elaboration of a chemical structures data base to be used in in silico studies; • to continue our current collaboration with Prof. Thomas Schmidt (natural products against neglected diseases – Phytochemistry and in silico methods); • to start a collaboration with Prof. A.G. Tempone (I.A. Lutz, BR) in the field of biological assays of pure compounds against Leishmania. 6. Evaluation of ResNet NPND activities, future perspectives and suggestions for improvement Please give a short statement describing your experiences with ResNet NPND, outline how you would imagine ResNet NPND in the future, including constructive suggestions for improvement. I enjoyed very much my participation as a member of the ResNet NPND in the field of natural products chemistry and chemoinformatics. It was a great opportunity to meet new scientists and to discuss with some of them about scientific projects as well as some interesting results in this field. During this period, I learnt a lot about this subject and could be aware about some problems related to neglected diseases that affect Brazil, including the state of Sao Paulo. Such contact gave m e more motivation to dedicate a substantial part of my research to this field. Some researchers of the network were very receptive and were always motivated to pursue scientific collaboration, while a few of them seemed to be not involved very much. In the future, I would imagine our network acting like a small factory, i.e., with natural products entering in one side and their biological activities and/or mechanism of action leaving the other side, involving the collaboration of researchers from different fields, especially parasite biochemistry and molecular biology. I would like to see the network responsible for providing pharma companies, government or academia at least a couple of hits or even lead compounds against neglected diseases. After that, other diseases such dengue or schistosomiasis could also be investigated. However, in order to achieve such results, the network must be visible to the world (scientific publications, meeting abstracts, local workshops, advertising in scientific journals and in the media) and its members should be involved and committed to its success, involving post-‐graduation students and financial support from financial agencies. 7. Confirmation of commitment, declaration of scientific independence and signature I hereby confirm that I renew my commitment myself to the aims and goals of ResNet NPND and that I wish to continue my membership in ResNet NPND. At the same time I declare, that I am legally authorized to conduct own research projects, coordinate joint research, publish data and work independently in a scientific environment. I understand that I have the right to terminate my membership at any time, which in this case I must do in written form, to a member of the executive board. Ribeirão Preto, 15 October 2013 ____________________________________________________________________ (Place) (Date) (Signature) Please fill in, print and sign this form. It can be sent back as hardcopy or, preferably, as a scanned pdf document to thomschm@uni-‐muenster.de ResNet
NPND
To all current members: Please fill in and send back by Oct. 15, 2013
Name de-Castro
First name: Solange L. Academic title(s): PhD
Institution: Fundação Oswaldo Cruz
Department: Lab. Biologia Celular- Instituto Oswaldo Cruz
Function: Titular Researcher
In the period 2011-2013 I am working with experimental chemotherapy of Chagas disease assaying only
synthetic compounds. I will begin now the investigation of compounds obtained from natural sources
Duszenko et al (2011) Autophagy in protists. Autophagy 7: 127-158
Soeiro MNC, De Castro SL (2011) Screening of potential anti-Trypanosoma cruzi candidates: In vitro and in vivo
studies. Open Med Chem J 5: 21-30.
Ferreira et al (2011) Synthesis and anti-Trypanosoma cruzi activity of β-lapachone analogues. Eur J Med Chem, 46:
3071-3077.
De Castro et al (2011) Experimental chemotherapy for Chagas disease: a morphological, biochemical and proteomic
overview of potential Trypanosoma cruzi targets of amidines derivatives and naphthoquinones. Mol Biol Int, ID
306928. Special IssueTarget Identification and Intervention Strategies against Kinetoplastid Protozoan
Parasites.
Daliry et al (2011) Trypanocidal activity of amidine compounds does not correlate with their binding affinity to
Trypanosoma cruzi kinetoplast DNA. Antimicrob Agents Chemotherapy, 55: 4765-4773.
Fraga et al (2011) Novel therapeutic strategies for Chagas` disease. In: Drug Development – A Case Study Based
Insight into Modern Strategies, Rundfeldt C (Ed), InTech, ISBN 978-953-307-257-9, cap. 16, 399-436.
Gonçalves et al (2011) A comparative assessment of mitochondrial function in epimastigotes and bloodstream
trypomastigotes of Trypanosoma cruzi. J Bioenerg Biomembr, 43: 651-661.
Fernandes et al (2012). A novel triazolic naphthofuranquinone induces autophagy in reservosomes and impairment
of mitosis in Trypanosoma cruzi. Parasitology, 139: 26–36.
Silva et al (2012) Acute experimental Trypanosoma cruzi infection: Establishing a murine model that utilises noninvasive measurement of disease parameters. Mem Inst Oswaldo Cruz, 107: 211-216.
Schmidt et al (2012) The potential of secondary metabolites from plants as drugs/leads against protozoan
neglected diseases – Part I. Hot topic issue: ‘Coming back to nature: plants as a vital source of pharmaceutically
important metabolites’. Curr Med Chem 19: 2128-2175.
Schmidt et al (2012) The potential of secondary metabolites from plants as drugs/leads against protozoan
neglected diseases - Part II. Hot topic issue: ‘Coming back to nature: plants as a vital source of pharmaceutically
important metabolites’. Curr Med Chem, 19: 2176-2228.
Silva Jr EN, et al (2012) On the search of potential anti-Trypanosoma cruzi drugs: Synthesis and biological evaluation
of 2-hydroxy-3-amino and 1,2,3-triazolic naphthoquinoidal compounds obtained from click reactions. Eur J Med
Chem, 52: 304-312.
Carvalho et al (2012) Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal
agents. Eur J Med Chem, 54: 512-521.
Borges-da-Silva et al (2013) Synthesis and trypanocidal activity of novel 2,4,5-triaryl-N-hydroxylimidazole
derivatives. Molecules 18:3445-3457;
De Castro et al (2013) Synthesis of Quinoidal Molecules: Strategies towards Bioactive Compounds with an Emphasis
on Lapachones. Eur J Med Chem, in press.
Diogo et al (2013) Synthesis and anti-Trypanosoma cruzi activity of naphthoquinone-containing triazoles:
Electrochemical studies on the effects of the quinoidal moiety. Bioorg Med Chem, in press.
Salomão et al (2013) Trypanosoma cruzi mitochondrial swelling and membrane potential collapse as primary
evidence of the mode of action of naphthoquinone analogues. BMC Microbiology, 13:196
Contribute to the development of new drugs for the treatment of Chagas disease studying synthetic
compounds and natural products.
Rio de Janeiro, September 20, 2013
(Place)
(Date)
(Signature)
Prof. Dr. João Henrique Ghilardi Lago
Institution: Universidade Federal de São Paulo (UNIFESP)
Department: Institute of Environmental, Chemical and Pharmaceutical Sciences
Function: Professor/Researcher
Our research group is involved in search of new antiparasital compounds from plant of
Brazilian biomes, mainly Cerrado (savanna like) and Atlantic Forest. Aiming this objective,
different plant species were collected in the above mentioned biomes and, based in
ethnopharmacological aspects, several were subjected to chromatographic procedures to
afford bioactive compounds. Thus, the obtained compounds could be used as prototypes to
development of new drugs to the treatment of antiparasital diseases, such as Leishmaniasis
and Chagas Disease.
1.
REA, A.; TEMPONE, A.G.; PINTO, E.G.; MESQUITA, J.T.; RODRIGUES, E.; SILVA, L.G.M.;
SARTORELLI, P.; LAGO, J.H.G. Soulamarin isolated from Calophyllum brasiliense (Clusiaceae)
induces plasma membrane permeabilization of Trypanosoma cruzi and mytochondrial
dysfunction, Plos Neglected Tropical Disease, submitted, 2013.
2.
MORAIS, T.R.; ROMOFF, P.; FAVERO, O.A.; REIMÃO, J.Q.; LOURENÇO, W.C.; TEMPONE, A.G.;
HRISTOV, A.D.; DISANTI, S.M.; LAGO, J.H.G.; SARTORELLI, P.; FERREIRA, M.J.P. Anti-malarial,
anti-trypanosomal and anti-leishmanial activities of jacaranone isolated from Pentacalia
desiderabilis (Vell.) Cuatrec. (Asteraceae). Parasitology Research, 110, 95-101, 2012.
3.
SARTORELLI, P.; SANTANA, J.S.; GUADAGNIN, R.C.; PINTO, E.G.; TEMPONE, A.G.; STEFANI, H.A.;
SOARES, M.G.; SILVA, A.M.; LAGO, J.H.G. In vitro trypanocidal evaluatioin of pinane derivatives
from essential oils of ripe fruits from Schinus terebinthifolius Raddi (Anacardiaceae). Química
Nova, 35, 743-747, 2012.
4.
GRECCO, S.S.; REIMÃO, J.Q.; TEMPONE, A.G.; SARTORELLI, P.; CUNHA R.L.O.R.; ROMOFF, P.;
FERREIRA, M.J.P.; FAVERO, O.A.; LAGO, J.H.G. In vitro antileishmanial and antitrypanosomal
activities of flavanones from Baccharis retusa DC. (Asteraceae). Experimental Parasitology, 130,
141-145, 2012.
5.
SCHMIDT, T.J.; KHALID, S.A.; ROMANHA, A.J.; ALVES, T.M.A.; BIAVATTI, M.A.; BRUN, R.; COSTA,
F.B.; CASTRO, S.L.; FERREIRA, V.F.; LACERDA, M.V.G.; LAGO, J.H.G.; LEON, L.L.; LOPES, N.P.;
AMORIM, R.C.N.; NIEHUES, M.; OGUNGBE, O.V.; POHLIT, A.M.; SCOTTI, M.T.; SETZER, W.N.;
SOEIRO, M.N.C.; STEINDEL, M.; TEMPONE, A.G. PART I - The potential of secondary metabolites
from plants as drugs or leads against protozoan neglected diseases. Current Medicinal
Chemistry, 19, 2128-2175, 2012.
6.
SCHIMIDT, T.J.; KHALID, S.A.; ROMANHA, A.J.; ALVES, T.M.A.; BIAVATTI, M.A.; BRUN, R.; COSTA,
F.B.; CASTRO, S.L.; FERREIRA, V.F.; LACERDA, M.V.G.; LAGO, J.H.G.; LEON, L.L.; LOPES, N.P.;
AMORIM, R.C.N.; NIEHUES, M.; OGUNGBE, O.V.; POHLIT, A.M.; SCOTTI, M.T.; SETZER, W.N.;
SOEIRO, M.N.C.; STEINDEL, M.; TEMPONE, A.G. PART II - The potential of secondary metabolites
from plants as drugs or leads against protozoan neglected diseases. Current Medicinal
Chemistry, 19, 2176-2228, 2012.
7.
SANTOS, R.T.F.; HIRAMOTO, L.L.; LAGO, J.H.G.; TEMPONE, A.G.; SARTORELLI, P. Antitrypanosomal activity of 1,2,3,4,6-penta-O-galloyl-β-D-glucose isolated from Plectranthus
barbatus Andrews (Lamiaceae). Química Nova, 35, 2229-2332, 2012.
8.
OLIVEIRA, A.; MESQUITA, J.T.; LAGO, J.H.G.; TEMPONE, A.G.; GUIMARÃES, E.F.; KATO, M.J.
Leishmanicidal activity of an alkenylphenol from Piper malacophyllum is related to plasma
membrane disruption. Experimental Parasitology, 132, 383-387, 2012.
9.
PASSERO, L.F.D.; BONFIM-MELO, A.; CORBETT, C.E.P.; LAURENTI, M.D.; TOYAMA, M.H.;
TOYAMA, D.O.; ROMOFF, P.; FÁVERO, O.A.; GRECCO, S.S.; ZALEWSKY, C.A.; LAGO, J.H.G. Antileishmanial effects of purified compounds from aerial parts of Baccharis uncinella C. DC.
(Asteraceae). Parasitology Research, 108, 529-536, 2011.
10. CORRÊA, D.S.; TEMPONE, A.G.; REIMÃO, J.Q.; TANIWAKI, N.N.; ROMOFF, P.; FÁVERO, O.A.;
SARTORELLI, P.; MECCHI, M.C.; LAGO, J.H.G. Anti-leishmanial and anti-trypanosomal potential
of polygodial isolated from stem barks of Drimys brasiliensis Miers (Winteraceae). Parasitology
Research, 109, 231-236, 2011.
11. GRECCO, S.S.; REIMÃO, J.Q.; TEMPONE, A.G.; SARTORELLI, P.; ROMOFF, P.; FERREIRA, M.J.P.;
FÁVERO, O.A.; LAGO, J.H.G. Isolation of an antileishmanial and antitrypanosomal flavanone
from the leaves of Baccharis retusa DC. (Asteraceae). Parasitology Research, 111-113, 2010.
Your research group is involved to discovery new prototypes compounds which could be used to
development of drugs based in natural products. Thus, our data could be useful in advanced studies
such as preparation of related compounds, aiming establish structure/activity relationships of bioactive
compounds or in the conduction of in vivo experiments aiming the evaluation of detected activity in
aminal models.
During the years of 2010 – 2013 our group reported in the literature the isolation of several compounds
from plant species of Brazilian biomes. Some of these compounds will be selected to conduct additional
experiments, such as chemical modification to increase activity and/or decrease cytotoxicity, with
support of Medicinal Chemists. However, will be interesting if the first task of ResNEt NPND was
directed to select two or three prototypes from a data base of results obtained from different
researches associated to this net aiming to conduct advanced studies (isolation on similar natural
compounds, chemical modification to preparation of analogs, structure/activity relationships and in vivo
evaluation).
São Paulo – September,18th, 2013.
____________________________________________________________________
(Place)
(Date)
(Signature)
Name Leitão
First name
Suzana
Academic title(s)PhD
Institution:Universidade Federal do Rio de Janeiro
Department: Departamento de Produtos Naturais e Alimentos
Function: Associate Professor
I have joined ResNet since the first meeting in 2011 and reportred some research with Brazilian medicinal
plants against malaria, tuberculosis and leishmaniosis that were originated from an ethnobotanical
research performed between 2006-2010 within Quilombola communities of Oriximina (North of Brazil).
Our research was the first one in Brazil to obtain approval from the Directing Council of Genetic Heritage
(Conselho de Gestão do Patrimônio Genético - CGEN) to access the traditional knowledge for
bioprospecting purposes. In that study, some plants were selected for bioassay-guided fractionation:
Ampelozizyphus amazonicus (against Malaria and Chagas disease) and two alkaloid rich species of
Aspidosperma (against malaria and TB). However, in 2012 we had to renew the approval (license) from
CGEN, and it took almost all 2012. In 2013 this new approval was released and we moved on with our
research with A. amazonicus. We reported its immunomodulatory properties, as well as studies by LCDAD-ESI-MS on its aqueous extracts. We are now working on screening some of the plant extracts
selected by ethnopharmacological approach (quantitative methodology) indicated for the treatment of
Leishmaniosis. Some of the plants listed in this ethnopharmacological survey have never been cited for
this purpose.
Articles related to Neglected Diseases, including TB (no articles co-authored by any members of
ResNet):
1. Vieira, MN, Porto, P C C, OLIVEIRA, D. R., PINTO, Shaft Corrêa, BRAZ-FILHO, R., Leitão,
Suzana Guimarães, LEITÃO, Gilda Guimarães. Application of pH-zone-refining countercurrent
chromatography for the separation of indole alkaloids from Aspidosperma rigidum Rusby.
Journal of Chromatography (Print). , v.1319, p.166 - 171, 2013.
2. Leitão, Fernanda, Leitão, Suzana Guimarães, Almeida, MZ, Cantos, Jessica, Coelho,
Tatiane S, SILVA, Pedro Eduardo de Almeida. Medicinal plants from open-air markets in the
State of Rio de Janeiro, Brazil as a potential source of new antimycobacterial agents. Journal of
Ethnopharmacology. , v.149, p.513 - 521, 2013.
3. Peçanha, Ligia M. Torres, FERNANDES, Patricia D, Simen , Tatiana Jotha-Mattos,
OLIVEIRA, D. R., Finotelli, Priscilla V., Pereira, MArina V A, Barboza, Fernanda F. , Almeida,
Thays S., Carvalhal, S. , Pierucci, Anna Paola T. R., LEITÃO, Gilda Guimarães, Rastrelli, Luca,
Piccinelli, Anna Lisa, Leitão, Suzana Guimarães. Immunobiologic and Antiinflammatory
Properties of a Bark Extract from Ampelozizyphus amazonicus Ducke. Journal of Biomedicine
and Biotechnology (Print). , v.2013, p.1 - 11, 2013.
4. Leitão, Fernanda, MOREIRA, D. L., Almeida, MZ, Leitão, Suzana Guimarães. Secondary
metabolites from the mistletoes Struthanthus marginatus and S. concinnus (Loranthaceae)..
Biochemical Systematics and Ecology. , v.48, p.215 - 218, 2013.
5. CASTELLAR, Aline, Coelho, Tatiane S., Silva, Pedro E. A., Ramos, Daniela F., Lourenço,
Maria Cristina S., Lage, Celso L. S., Julião, Lisieux S., Barbosa, Ymira G., Leitão, Suzana
Guimarães. The activity of flavones and oleanolic acid from Lippia lacunosa against susceptible
and resistant Mycobacterium tuberculosis strains. Revista Brasileira de Farmacognosia
(Impresso). , v.21, p.835 - 840, 2011.
6. Oliveira, Danilo R., Leitão, Gilda G., Coelho, Tatiane S., Silva, Pedro E. Almeida da,
Lourenço, Maria Cristina S., Leitão, Suzana Guimarães. Ethnopharmacological versus random
plant selection methods for the evaluation of the antimycobacterial activity. Revista Brasileira de
Farmacognosia (Impresso). , v.21, p.793 - 806, 2011.
Book Chapter:
1. OLIVEIRA, D. R., LEITÃO, Gilda Guimarães, Castro, N.G., Vieira, MN, ARQMO, Leitão,
Suzana Guimarães. Ethnomedical Knowledge among the “Quilombolas” from the Amazon
Region of Brazil with a Special Focus on Plants Used as Nervous System Tonics In: Medicinal
Plants: Biodiversity and Drugs.1 ed.Enfield, New Hampshire : Science Publishers, 2012, v.01, p.
142-178.
with ResNet NPND.
I wish to continue as a member of this net because I believe that I can contribute to the discovery of new
prototypes for Leishmaniosis treatment from natural sources, originated from plants traditionally used
by quilombola communities. Some of the plants listed in this ethnopharmacological survey have never
been cited for this purpose.
I joined this network looking for cooperation with Brazilian and other foreign researchers to look for
secondary metabolites active against Neglected diseases: Leishmaniosis and Chagas Disease. I have set
collaboration with some members for phytochemical (Gerold Jertz and Adrian M. Pohlit) work and hope
to begin now the collaboration with FIOCRUZ, Rio de Janeiro, to screen plant extracts from
ethnopharmacological study against Leishmaniosis. My suggestions for improvement and maintenance
of the ResNet is, when possible, to organize meetings where member can present their achievements
within the net.
_Rio de Janeiro, March 6th, 2014
(Place)
(Date)
(Signature)
Questionnaire for ResNet NPND members’ report To all current members: Please fill in and send back by Oct. 15, 2013 1. Personal information Name Lopes First name Norberto Peporine Academic title(s) Professor in Organic Chemistry 2. Affiliation – Institution, Department, Function Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, University of São Paulo Department: Physic and Chemistry Function: Full Professor in Organic Chemistry and Head of the Department 3. Report on activities in and for ResNet NPND since April 2011 During this period our group selected some active natural products to development a plataform of preclinical trials. The selected compound were submitted to biomimetic studies, in which the jacobsen's catalyst was introduced instead of the more common metalloporphyrins, herewith achieving for biomimetic reactions very high yields. In several cases the yields of catabolized active compounds exceeded 90%, which is extremely significant. These main products obtained by biomimetic reactions were the same as observed in the microsomal metabolism. This enabled the perspective of producing phase one metabolites for further pharmacokinetic analysis. The fragmentation studies in gas phase allowed the definition of complete pathways from three classes of natural products with anti-‐parasite activity. The first pharmacokinetic pilot study clarified the elimination mechanism and half life time of a tripanocidal lignan. These results show the viability of the proposal and generate the expectation of better understanding the absorption, distribution and metabolization mechanism for selected active natural products. 4. Publications relevant to the field 1. DA COSTA, RAPHAELLA CORREIA ; SANTANA, DANDARA BRAGA ; ARAÚJO, RENATA MENDONÇA ; DE PAULA, JOSÉ ELIAS ; DO NASCIMENTO, PATRÍCIA COELHO ; Lopes, Norberto Peporine ; BRAZ-‐
FILHO, RAIMUNDO ; ESPINDOLA, LAILA SALMEN . Discovery of the rapanone and suberonone mixture as a motif for leishmanicidal and antifungal applications. Bioorganic & Medicinal Chemistry (Print), v. 22, p. 135-‐140, 2014. 2. SARTORI, LUCAS ROSSI ; Vessecchi, Ricardo ; Humpf, Hans-‐Ulrich ; DA COSTA, FERNANDO BATISTA ; Lopes, Norberto Peporine . A systematic investigation of the fragmentation pattern of two furanoheliangolide C-‐8 stereoisomers using electrospray ionization mass spectrometry. RCM. Rapid Communications in Mass Spectrometry, v. 28, p. 723-‐730, 2014. 3. GUARATINI, Thais ; SILVA, D. B. ; BIZARO, ALINE CAVALLI ; SARTORI, L. R. ; Humpf, Hans-‐Ulrich ; LOPES, N. P. ; LOTUFO, Letícia Veras Costa ; LOPES, João Luis Callegari . In vitro metabolism studies of erythraline, the major spiroalkaloid from Erythrina verna. BMC Complementary and Alternative Medicine (Online), v. 14, p. 1-‐5, 2014. 4. MESSIANO, GISELE BARALDI ; SANTOS, RENAN AUGUSTO DA SILVA ; FERREIRA, Leandro de Santis ; SIMÕES, RODRIGO ALMEIDA ; JABOR, VALQUÍRIA APARECIDA POLISEL ; KATO, Massuo Jorge ; Lopes, Norberto Peporine ; PUPO, Mônica Tallarico ; DE OLIVEIRA, ANDERSON RODRIGO MORAES . In vitro metabolism study of the promising anticancer agent the lignan (−)-‐grandisin. Journal of Pharmaceutical and Biomedical Analysis (Print), v. 72, p. 240-‐244, 2013. 5. Vessecchi, Ricardo ; Emery, Flavio S. ; LOPES, N. P. ; Galembeck, Sérgio E. . Eletronic structure and gas-‐phase chemistry of protonated α-‐and β-‐quinonoid compounds: a mass spectrometry and computational study. RCM. Rapid Communications in Mass Spectrometry, v. 27, p. 816-‐824, 2013. 6. BREITBACH, ULRIKE B. ; Niehues, Michael ; Lopes, Norberto P. ; FARIA, JAIR E.Q. ; BRANDÃO, MARIA G.L. . Amazonian Brazilian medicinal plants described by C.F.P. von Martius in the 19th century. Journal of Ethnopharmacology, v. 147, p. 180-‐189, 2013. 7. SILVA, EVERTON M. ; ARAÚJO, RENATA M. ; FREIRE-‐FILHA, LINDOMAR G. ; SILVEIRA, EDILBERTO R. ; Lopes, Norberto P. ; PAULA, JOSÉ ELIAS DE ; BRAZ-‐FILHO, RAIMUNDO ; Espindola, Laila S. . Clusiaxanthone and Tocotrienol Series from Clusia pernambucensis and their Antileishmanial Activity. Journal of the Brazilian Chemical Society (Impresso), v. 24, p. 1314-‐1321, 2013. 8. LOPES, ADRIANA A. ; PINA, EDIEIDIA S. ; SILVA, DENISE B. ; PEREIRA, ANA MARIA S. ; DA SILVA, MARIA FÁTIMA DAS G. F. ; DA COSTA, FERNANDO B. ; Lopes, Norberto P. ; Pupo, Mônica T. . A biosynthetic pathway of sesquiterpene lactones in Smallanthus sonchifolius and their localization in leaf tissues by MALDI imaging. Chemical Communications (London. 1996. Print), v. 49, p. 9989, 2013. 9. SCHMIDT, T. J. ; DA COSTA, F. B. ; LOPES, N. P. ; KAISER, M. ; BRUN, R. . In Silico Prediction and Experimental Evaluation of Furanoheliangolide Sesquiterpene Lactones as Potent Agents against Trypanosoma brucei rhodesiense. Antimicrobial Agents and Chemotherapy (Online), v. 58, p. 325-‐332, 2013. 10. Basset, Charlie ; Rodrigues, Alice M.S. ; Eparvier, Véronique ; Silva, Maria R.R. ; Lopes, Norberto P. ; Sabatier, Daniel ; Fonty, Emile ; Espindola, Laila S. ; Stien, Didier . Secondary metabolites from Spirotropis longifolia (DC) Baill and their antifungal activity against human pathogenic fungi. Phytochemistry, v. 74, p. 166-‐172, 2012. 11. Schmidt TJ, ; Khalid SA ; Romanha AJ ; Alves TM ; Biavatti MW, ; Brun R ; COSTA, Fernando Batista da ; de Castro SL ; Ferreira VF ; de Lacerda MV ; Lago JH ; Leon LL ; LOPES, N. P. ; das Neves Amorim RC ; NIEHUES, M. ; Ogungbe IV ; Pohlit, Adrian Martin ; Scotti MT ; Setzer WN ; Soeiro MD ; Steindel M ; Tempone AG . The Potential of Secondary Metabolites from Plants as Drugs or Leads Against Protozoan Neglected Diseases -‐ Part I. Current Medicinal Chemistry, v. 19, p. 2128-‐2175, 2012. 12. Schmidt TJ, ; Khalid SA ; Romanha AJ ; Alves TM ; Biavatti MW, ; Brun R ; COSTA, Fernando Batista da ; de Castro SL ; Ferreira VF ; de Lacerda MV ; Lago JH ; Leon LL ; LOPES, N. P. ; das Neves Amorim RC ; NIEHUES, M. ; Ogungbe IV ; Pohlit, Adrian Martin ; Scotti MT ; Setzer WN ; Soeiro MD ; Steindel M ; Tempone AG . The Potential of Secondary Metabolites from Plants as Drugs or Leads Against Protozoan Neglected Diseases -‐ Part II. Current Medicinal Chemistry, v. 19, p. 2176-‐2228, 2012. 13. SOUSA, JOÃO PAULO BARRETO ; TOMAZ, José Carlos ; DA SILVA, CECILIA C.P. ; ELLENA, JAVIER ; Lopes, Norberto Peporine ; LOPES, João Luis Callegari . Novel sesquiterpene lactones from Eremanthus seidelii. Tetrahedron Letters, v. 53, p. 6339-‐6342, 2012. 14. FEITOSA, LUÍS GUILHERME PEREIRA ; GUARATINI, Thais ; LOPES, João Luis Callegari ; Lopes, Norberto Peporine ; BIZARO, ALINE CAVALLI ; Silva, Denise Brentan da . Aplicação de espectrometria de massas com ionização por elétron na análise de alcaloides do mulungu. Química Nova (Impresso), v. 35, p. 2177-‐2180, 2012. 15. SOARES, ANA CAROLINA FERREIRA ; SILVA, ALINE NAZARÉ ; MATOS, PRISCILLA MENDONÇA ; SILVA, EDER HENRIQUE DA ; HELENO, Vladimir Constantino Gomes ; Lopes, Norberto Peporine ; LOPES, João Luis Callegari ; SASS, DAIANE CRISTINA . Complete H and 13C NMR structural assignments for a group of four goyazensolide-‐type furanoheliangolides. Química Nova (Impresso), v. 35, p. 2205-‐2209, 2012. 16. VESSECCHI, Ricardo Lourenço ; Emery, Flavio S. ; GALEMBECK, Sérgio Emanuel ; Lopes, N.P. . Gas-‐
phase reactivity of 2-‐hydroxy-‐1,4-‐naphthoquinones: a computational and mass spectrometry study of lapachol congeners. Journal of Mass Spectrometry (Print), v. 47, p. 1648, 2012. 17. Niehues, Michael ; BARROS, VALÉRIA PRISCILA ; EMERY, FLÁVIO DA SILVA ; DIAS-‐BARUFFI, MARCELO ; Assis, Marilda das Dores ; Lopes, Norberto Peporine . Biomimetic in vitro oxidation of lapachol: A model to predict and analyse the in vivo phase I metabolism of bioactive compounds. European Journal of Medicinal Chemistry, v. 54, p. 804-‐812, 2012. 18. DE SANTIS FERREIRA, LEANDRO ; CALLEJON, DANIEL ; ENGEMANN, ANNA ; Cramer, Benedikt ; Humpf, Hans-‐Ulrich ; DE BARROS, VALÉRIA ; ASSIS, MARILDA ; DA SILVA, DENISE ; DE ALBUQUERQUE, SÉRGIO ; OKANO, LAURA ; KATO, MASSUO ; LOPES, NORBERTO . In vitro Metabolism of Grandisin, a Lignan with Anti-‐chagasic Activity. Planta Medica, v. 78, p. 1939-‐
1941, 2012. 19. Pohlit, Adrian ; LOPES, N. P. ; Gama, Renata ; Tadei, Wanderli ; de Andrade Neto, Valter . Patent Literature on Mosquito Repellent Inventions which Contain Plant Essential Oils -‐ A Review. Planta Medica, v. 77, p. 598-‐617, 2011. 20. Pohlit, Adrian ; Rezende, Alex ; Lopes Baldin, Edson ; LOPES, N. P. ; de Andrade Neto, Valter . Plant Extracts, Isolated Phytochemicals, and Plant-‐Derived Agents Which Are Lethal to Arthropod Vectors of Human Tropical Diseases -‐ A Review. Planta Medica, v. 77, p. 618-‐630, 2011. 21. MACHADO, F. L. S. ; Pacienza-‐Lima, W. ; ROSSI-‐BERGMANN, B. ; GESTINARI, L. M. S. ; FUJII, M. T. ; PAULA, J. C. ; COSTA, Sônia Soares ; LOPES, N. P. ; KAISER, C. R. . Antileishmanial sesquiterpenes from the brazilian red alga Laurencia dendroidea. Planta Medica, v. 77, p. 733-‐735, 2011. 22. Vessecchi, Ricardo ; NAAL, Zeki ; LOPES, José Norberto Callegari ; GALEMBECK, Sérgio Emanuel ; LOPES, N. P. . Generation of Naphthoquinone Radical Anions by Electrospray Ionization: Solution, Gas-‐Phase, and Computational Chemistry Studies. The Journal of Physical Chemistry. A, p. 110511140346028-‐5460, 2011. 23. Sass, Daiane C. ; Heleno, Vladimir C. G. ; Morais, Gustavo O. ; Lopes, João L. C. ; LOPES, N. P. ; Constantino, Mauricio G. . Selectivity in reduction of natural furanoheliangolides with Stryker's reagent. Organic & Biomolecular Chemistry, v. 9, p. 6148-‐6153, 2011. 24. VESSECCHI, Ricardo Lourenço ; LOPES, José Norberto Callegari ; LOPES, N. P. ; Galembeck, Sérgio E. . Application of the Atoms in Molecules Theory and Computational Chemistry in Mass Spectrometry Analysis of 1,4-‐Naphthoquinone Derivatives. The Journal of Physical Chemistry. A, v. 115, p. 12780-‐12788, 2011. 5. Motivation to continue membership I’m very interest to introduce some of the activity compounds (select by the net) in the pre-‐clinical platform based on FCFRP-‐USP. 6. Evaluation of ResNet NPND activities, future perspectives and suggestions for improvement My experience with networks in Brazil, made me realize that the work progressed only when the coordinator defined groups and objectives. As an example the choice of a group of molecules for all work. So my suggestion would be that the network coordinator decided who would work with that. 7. Confirmation of commitment, declaration of scientific independence and signature I hereby confirm that I renew my commitment myself to the aims and goals of ResNet NPND and that I wish to continue my membership in ResNet NPND. At the same time I declare, that I am legally authorized to conduct own research projects, coordinate joint research, publish data and work independently in a scientific environment. I understand that I have the right to terminate my membership at any time, which in this case I must do in written form, to a member of the executive board. Ribeirão Preto, 13/03/2014 ____________________________________________________________________ (Place) (Date) (Signature) Please fill in, print and sign this form. It can be sent back as hardcopy or, preferably, as a scanned pdf document to thomschm@uni-‐muenster.de Questionnaire for ResNet NPND members’ report
Name Scotti
First name
Marcus
Academic title(s) Prof.
Institution: Federal University of Paraíba
Department: Engineering and environment
Function:Professor




Presentation: “Molecular Descriptors in QSAR of Potential Antiprotozoal Compounds” Seminal Workshop: “Research Initiative on Natural Products against Neglected
Diseases” Date: April 26-28, 2011 (Organizer: Prof. Dr. T. J. Schmidt)
Workshop: Research Network Natural Products against Neglected Diseases
Coordination of the Project: VIRTUAL SCREENING OF NATURAL PRODUCTS MAINLY
ISOLATED FROM ASTERACEAE AND APOCYNACEAE FAMILIES WITH LEISHMANICIDAL
AND TRYPANOCIDAL ACTIVITIES.
Developing a web tool to share and extract information from structures of secondary
metabolites, botanical occurrences, biological activities and others experimental data.
One manuscript submitted to Chemometrics and Intelligent Laboratory Systems.
Abstracts:
 Fast virtual screening of alkaloids from Apocynaceae with potential antitrypanosomal
activity. Marcus T. Scotti, Marcelo Sobral da Silva, Luciana Scotti. 8th Colloquium
Chemiometricum Mediterraneum (CCM VIII 2013)

Fast virtual screening of sesquiterpene lactones from Asteraceae with potential
antileishmanial activity. Scotti, MT; da Silva, MS; Pitta, IR; Speck-Planche, A; Scotti, L:
61st International Congress and Annual Meeting of the Society for Medicinal Plant and
Natural Product Research
It is an opportunity to share studies with several other researchers and apply the knowledge in
a net with several researches. Particularly I am very interested in methods of Virtual screening
and development tool to share data and extract information.
I think that we could spend more energy to increase the cooperation between the members,
then we will have more studies published with more than one researcher, but mainly share data
and in this way, it will be more effective to extract interesting information for the net. I think that
these reports periodically will help to monitor the activities of the net, too. In my opinion the need
to report periodically some activities will increase the amount of results and of course
publications, in other way the researches will spent more time in other priorities, colaborations,
personal projects, etc.
Setzer
Name
William
First name
Professor
Academic title(s)
Institution: University of Alabama in Huntsville
Department: Department of Chemistry
Function:
I have an ongoing collaboration with Prof. Ifedayo Victor Ogungbe (Department of Chemistry, Jackson
State University, Mississippi, USA) on in-silico evaluation of antiparasitic natural products with parasite
target proteins.
I have an ongoing collaboration with Dr. Lianet Monzote (Pedro Kouri Institute of Tropical Medicine,
Cuba) on antileishmanial natural products, isolation and structure elucidation.
“Comparative chemical, cytotoxicity, and antileishmanial properties of essential oils from Chenopodium
ambrosioides.” Monzote, L.; Nance, M.R.; García, M.; Scull, R.; Setzer, W.N. Natural Product
Communications, 2011, 6, 281-286.
“Prenylated isoflavonoids from Rhynchosia edulis.” Ogungbe, I.V.; Hill, G.M.; Crouch, R.A.; Vogler, B.;
Nagarkoti, M.; Haber, W.A.; Setzer, W.N. Natural Product Communications, 2011, 6, 1637-1644.
“Antileishmanial natural products from plants.” Ogungbe, I.V.; Singh, M.; Setzer, W.N. Studies in
Natural Products Chemistry: Bioactive Natural Products, 2012, 36, Chapter 10 (invited book chapter),
331-382.
“In-silico investigation of antitrypanosomal phytochemicals from Nigerian medicinal plants.” Setzer,
W.N.; Ogungbe, I.V. PLoS Neglected Tropical Diseases, 2012, 6(7), e1727.
“Docking of antischistosomal natural products with relevant protein targets.” Setzer, W.N. Advances in
Chemistry Research, 2012, 16, 185-205.
“Antiprotozoal activity of essential oils.” Monzote, L.; Alarcón, O.; Setzer, W.N. Agriculturae
Conspectus Scientificus, invited review, 2012, 77(4), 167-175.
“In-silico Leishmania target selectivity by antiparasitic terpenoids.” Ogungbe, I.V.; Setzer, W.N.
Molecules, 2013, 18, 7761-7847 (Special Issue, Plant Natural Products against Human
Parasites).
“Interactions of antiparasitic alkaloids with Leishmania protein targets: A molecular docking
analysis.” Ogungbe, I.V.; Ng, J.D.; Setzer, W.N. Future Medicinal Chemistry, 2013, 5(15), 17771799.
“Antileishmanial phytochemical phenolics: Molecular docking to potential protein targets.”
Ogungbe, I.V.; Erwin, W.R.; Setzer, W.N. Journal of Molecular Graphics & Modelling, 2014, 48,
105-117.
I think this is a potentially very valuable extended collaboration, and I would like to continue to
participate.
My participation has been, unfortunately, minimal. I was unable to attend either of the meetings in
Germany due to situations outside my control. For me, the best improvement is for me to attend the
next meeting.
Huntsville, Alabama
March 1, 2014
____________________________________________________________________
(Place)
(Date)
(Signature)
"
Questionnaire for ResNet NPND members' report
To ali current members: Please fill in and send back by Oct. 15.2013
1.
Personal information
Name
2.
Soeiro
Academic title(s): pHD
Affiliation -Institution,
First name Maria de Nazaré Correia
Department, Function
Institution: Instituto Oswaldo Cruz - Fiocruz
Department: Laboratório de Biologia Celular
Function: Head of the Laboratório de Biologia Celular - Titular Reseacher
3.
Report on activities in and for ResNet NPND since April 2011
In vitro and in vitro studies have been conducted with the RESNet partners and two papers recently
published (1. Effects of psilostachyin A and cynaropicrin against Trypanosoma cruzi in vitro and in vivo.
da Silva CF, Batista DD, Siciliano JA, Batista MM, Lionel J, de Souza EM, Hammer ER, da Silva PB, De Mieri
M, Adams M, Zimmermann S, Hamburger M, Brun R, Schühly W, Soeiro MD.
Antimicrob Agents Chemother. 2013 Aug 12. {Epub ahead of print] and 2. In vitro and in vivo activity of
the chloroaryl-substituted
imidazole viniconazole against Trypanosoma cruzi. CRISTlANEFRANÇA DA SIL,
DENISE DA GAMA JAEN BATlSTA, MARCOS MEUSER BATlSTA, JESSICALlONEL, ERICA RIPOLL HAMMER,
RETO BRUN and MARIA DE NAZARÉ CORREIASOEIRO, Laboratório de Biologia Celular, Fundação
Oswaldo Cruz, Rio de Janeiro, RJ, BraziL, Department of Medical Parasitology and Infection Biology, Swiss
Tropical and Public Health tnstitute, Baset, Switzerland (Received 21 May 2013; revised 25 June and 13
August 2013; accepted 15 August 2013 -Parasitology -In press.
4.
-~-------
-
Publications relevant to the field
-
~~--
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Please give full bibliography
authored
1.
011 your scientific
of
by at least ane further
member
G, Hargrove
TY, Waterman
10.1128/AAC00070-13.
Inhibitar
Orug-Resistant
of whether
GI.Antimicrob
Agents
Chemother.
17. In Vitro and In Vivo Studies afthe
Strains
and 2013. Please mork those that were co-
vau made an acknowledgement
ta ResNet NPNO, or not}.
G, Batista MM, Pavão BP, Araújo JS, Aiub CA, da Silva PB, Lionel J, Britta C, Kim K,
Oda
Mf/, tepesnevo
Epub 2013 Jun
VNI against
to the fieid in the years 2011,2012
relevant
Soeiro Mde N, de Souza EM, da Silva CF, Batista
Sulikowski
2.
pubtications
of ResNet NPNO in red (irrespective
ofTrypanosoma
2013 Sep;57(9):4151-63.
Antiparasitic
Activity
doi:
ofSteroll4a-Oemethylase
(CYP51)
cruzi.
00, Siciliano JA, Batista MM, Lionel J, de Souza EM, Hammer ER, da Silva PB, De Mieri M, Adams M, Zimmermann
5,
M, Brun R, Schühly W, Soeiro MO. Effects of psifostachyin A and cynaropicrin against Trypanosama cruzi in vitro and in vivo.
Antimicrob
Agents Chemather.
2013 Aug 12. [Epub ahead of print]
CRISTIANE FRANÇA DA SIL, DENISE DA GAMA JAEN BATISTA, MARCOS MEUSER BATISTA, JESSICA LfONEL, ERICA RIPOLL HAMMER, RETO
da Silva CF, Batista
Hamburger
3.
BRUN and MARIA DE NAZARÉ CORREIA SOEIRO In vitro and in vivo activity
Trypanosoma
4.
5.
cruzi.,2013
- Parositology
K, Boykin OW, Wifson
intracellular
a systematic
Ligiane
porosites:
R. Gouveo,
and the biological
Parasitology.
Denise da Gama Jean Batista,
Zn(II)-based
against
Bernardina;
ZONGYING;
Correia.
Trypanosoma
cruzi.
Oaliry, Anissa ; Aroujo,
BioMetals
Trypanosoma
cruzi Infection.
ofthe
PIos One, v.
Ti; Khalid SA ; Romanha
Julianna
Efftcocy
October
Oliveira,
5icifiana
A; KUMAR, ARVINO;
FARAHAT, ABOELBASSET
Maria
aciâ base ionization
complexes:
In Vitro and In Vivo Investigation
Schmidt
ANovel
amidines
2013 Jul;140(8):929-51.
DA 5ILVA, CRISTlANE FRANÇA BATISTA, Denise da Gama Jaen;
Sifva, Patricia
7.
effec:
WO, Wang MZ, Hemphifl
review.
A Martins,
Darliane
of the chloroaryl-substituted
imidazole
viniconazole
against
press.
Soeiro MN, Werbovetz
tetkio R. Teixeira. Norfloxacin
6.
-In
determination,
2013,
Volume
Gabriel
MeIo;
David
agents
against
de Souza, Elen Mello;
Constança;
DB1831
DNA and albumin
binding
properties
26, Issue 5, pp 813-825
Rodrigues,
W.; de Nazaré
of Arylimidamide
as promising
C Sceiro, Sonia R. W. Louro, Paulo J. S. Barbeiro,
de Nazaré
constant
; Britto,
Boykin,
ond analogues
doi: 10.1017/50031182013000292.
Hammer,
Ana Carolina
Correia soetro,
and Its Mesylated
Erica Ripoll;
Mondaine
Maria;
Soeiro, Maria
Salt Form - DB1965
da
; LfU,
de Nazaré
- against
7, p. e30356, 2012.
Biavatti MW ; Brun R; Da Costa FB ; De Castro SL ; Ferreiro VF; Lacerda MVG ; Lago
RC; Niehues M; Ogungbe IV; Pohlit AM ; Scotti MT ; Setzer WN ; de Nazare C Soeiro M;
Ai ; Alves TMA;
1HG; Leon LL; Lopes NP; Neves Amorim
M ; Tempone AG. The potential of secondary metabolites from plants as drugs/leads against protozoan neglected diseases Part
back to nature: plants as a vital source of pharmaceutically
important
metobolltes.
Current Medicinal
Chemistry, v. 19, p. 2128-2175, 2012.
Steindel
I. Hot tooic issue: Coming
8.
Schmidt
TJ; Khalid SA; Romanha
Ai;
Alves TMA;
A; Neves Amorim
Biavatti
MW;
Brun R; Da Costa FB; de Castro, Solange
2176-2228,
9.
Werbovetz,
Setzer WN;
VF; Lacerda
MVG;
Soeiro
S. ; Parman,
(Print],
v.
Disease:
In Vivo Efftcacy, Acute
56, p. 3690-3699,
Toxicity,
Pharmacokinetics,
and Toxicology
Studies. Antimicrobial
Agents
and
2012.
Denise; Sifva, Patrícia Bernardino;
Louro, Sonia R. w.; Nazaré C Soeiro,
C. Copper(lI) fluoroquinolone
complexes with onti- Trypanosoma
cruzi activity and
DNA binding abifity. BioMetals
(Oxford}, v. 25, p. 633-645, 2012.
HARGROVE, TATlANA Y.; SOEIRO, M.N. C; BATISTA, O.G.1.; de Nazaré Correia Soeiro, Maria;
DA SILVA, CRISTlANE FRANÇA; tepesheva,
Galina I. ; Yaüovitskayo, Eugenio M. ; da Gama Jaen Batista, Denise; Kim, Kwangho;
Waterman,
Michael R. ; Sulikowski, Gary A. ;
Martins,
Darliane
Maria;
A ; Gouvea,
Teixelra,
iiqione
Letícia R. ; Soeiro,
BATISTA, Marcos
Meuser.
InternationalJournol
R. ; Gama Jean Batista,
Maria
activity
development
in vitro of aromatic
v.
v.
of novei, pathogen-specific
amidine
inhibitory
scaffolds.
2, p. 178-186,2012.
AS.G.; Ismaif, MA; Arafa, R.K.; Toa, B.; Nixon-Smitn,
Nefertiti,
Parasitology,
and structure-based
Drugs and Drug Resistance,
and selectivity
cruzi. Experimental
de Nazaré
CYP51 structures
for Parasitology:
De Souza, EM.; da Silva, P.B.;
Trypanocidal
13.
MT;
O.; STEPHENS,
and Chagas'
Chemotheropy
12.
Scotti
T.; Green, C E. ; Mirsalis, J. C ; de Nazare Correia soeiro, M. ; Mello de Souza, E. ; Da Sifva, C F. ; da
C E; Banerjee, M.; Farahat, A A.; Munde, M.; Wilson, W. D.; BOYKIN, D. W.; Wang, M. z.,
K. A ; Soeiro, Maria de Nazaré C. Evaluation of Arylimidamides
OB1955 and DB1960 as Candidates against Viscerol
t.elsnmaniasis
11.
IV; Pohlit AM;
2012.
Zhu, X. ; Liu, Q. ; Yang,
Gama Jaen Batista,
10.
RC; Niehues
M; Ogungbe
L.; Ferreiro
M ; Steindel M;
Tempane AG . The potentiol
of secondary metabafites
from plants as drugs/leads
against protozoan
neglected diseases - Part 11.Hat topic
issue: Coming back to nature: plants as a vital source of pharmaceutically
important
metabolites
. Current Medicinal
Chemistry, v. 19, p.
Lago 1HG; Leon LL; LOPES,
compounds
upon bloodstream
CK.;
BOYKIN, D.w.;
and introcellular
forms
Soeiro,
M.N.C.
of Trypanosoma
127, p. 429435, 2011.
A; Lima MM; Romanho
À1; Soles Junior PA; Stephens CE; SOM, P.; David W; Soeiro, Maria de
C. In vitro Trypanocidal Activity of DB745B and Other Novel Arylimidamides
Against Trypanosoma
cruzi. Journal of Antimicrobial
Chemotherapy
(Print), v. 66, p. 1295-1297, 2011.
SOEIRO, M. N. C ; CASTRO, S. L. . Screening of Potential onti- Trypanosoma
cruzi Candidates: In Vitro and In vivo. The Open Medicinal
ChemistryJournal,
v. 5, p. 21-30, 2011.
BATISTA, D. DA G. J.; Sifva, Patricia Bernardino
do; Stivanin L; Lachter DR; Sifva RS; Teixeira LR; Soeiro, Maria de Nazaré Correia. Co(II),
SILVA, Cristiane
França da; Junqueira
Nazaré
14.
15.
Mn(lI)
and Cu(lI) complexes
Polyhedron,
16.
de Castro, Solange
Rubem F.
17.
Batista,
M.;
and Benznidazole
da Silva de Azevedo
Herbert
B. ; Schorfstein,
endothelin
Biochemical,
and biologicol
evaluation
Serra, Rafaela
Meuser;
against
Trypanosoma
cruri .:
Soelro,
Rangel;
Maria
and Proteomic
tntemationat,
Oliveira,
Gabriel
Daliry, Anissa ; de Souza, Elen M. ; Menna-Barreto,
B.; Soelro,
Overview
v. 2011, p.
MeIo de;
Maria
SvensjÃ,
de Nazaré
a converging
Erik;
Ana Carolina;
Correia.
pathway
de AroÃ"jo
Trypanosoma
cruzi Targets
Britto,
Constança
Lima, Ana Paulo Cabral;
cruzi invades
to chagasic
of
1-13, 2011.
Carvalho;
Rodrigues,
Treatment
Junlor,
Ana
of Heterocycfic
Erivan Schnaider
verk'rüca ; de NazarÃ Correia Soeiro, Maria;
Morandi,
Trypanosoma
leading
C . Experimental
de Nazaré
of Potentiol
W. ; Soelro, Maria de Nazaré Correia. Combined
cruzi In Vivo. PIos One, v. 6, p. e22155, 2011.
J
receptors:
Biology
Wanderson;
F.; Sifva, Patricia
David
Fabio; de Faria Morandini
Julio;
and bradykinin
Molecular
upon Trypanosoma
Fortes,
studies
M. ; Batista,
A Morphologicol,
Chad E. ; Boykin,
Daniele;
Marcos
Silva, Cristiane
BATISTA, Marcos
Stephens,
dos Santos Andrade,
spectroscopicol
Kelly;
and Naphthoquinones.
Mondaine;
Analogues
Salomão,
for Chagas Disease:
Denise da Gama Jaén;
Carolina
18.
Denise G. J. ; Batista,
Gabriel
Derivatives
synthesis
2011.
L. ; Batista,
S. ; Oliveira,
Chemotherapy
Amidines
cf fluorquinolones:
v. 30, p.1718-1725,
host cells through
vasculopathyâ
the activation
. British Journal
Ramos;
Tanowitz,
of
of Pharmacology,
p. no-
no, 2011.
19.
õotiry,
A.; Pires, M. Q.; Sifva, C F. ; Pacheca, R. S. ; Munde, M.; STEPHENS, C E. ; KUMAR, A.; ISMAIL, M. A; tiu, z.. Farohat, A. A.;
Q.; BOYKIN, D. w.. Wifson, W. D.; De Castro, S. L.; Soelro, M. N. C; soeiro, Maria de Nazaré Correia. The
AKAY, S.; SOM, P.; HU,
20.
Trypanocidal
Activity
of Amidine
Antimicrobial
Agents
ond Chemotherapy
DA SILVA, CRISTlANE FRANÇA;
ABDELBASSET
Compounds
Does Not CorreIa te with Their Binding
(Print),
Daliry, Anissa;
v.
DA SILVA, PATRíCIA BERNARDINO;
A. ; FISHER, MARY K.; HU, LAIXING;
SOEfRO, MARIA DE NAZARÉ;
Soeiro, Maria
Parasitology
v.
(London.
Print],
Affinity
to Trypanosoma
cruzi Kinetoplast
DNA.
55, p. 4765-4773, 2011.
KUMAR,
de Nazaré
ARVIND;
Correia.
138, p. 1863-1869, 2011.
AKAY, SENOL; BANERJEE, MOLOY;
LfU, ZONGYING;
The efficacv
Stephens,
of novei orylimidamides
Chad
FARAHAT,
E; Boykin, David W. ; CORREIA
against
Trypanosoma
cruzi in vitro.
5.
Motivation to continue membership
Please give a short statement explaining whV VOUwish to continue your membership and coaperation
with ResNet NPND.
,
Contribute for research knowledge and technical development of novel therapeutic options for treating
neglected diseases of the poverty.
6.
Evaluation of ResNet NPND activities, future perspectives and suggestions for improvement
Please give a short statement describing your experiences with ResNet NPND, outline how Vou would
imagine ResNet NPND in the [uture, including constructive suggestions for improvement.
-more interactive regular meetings (Iike teleconferences) and search for international supports to
improve the NPND interaction and activities.
7.
Confirmation
of commitment,
declarati9n of scientific independence and signature
/ hereby confirm that 1renew my commitment myse/j to the aims and goals of ResNet NPND and that 1
At the same time 1declare, that 1amJegally authorized to conduct own research projects, coordinate
joint research, publish data and work independent/y in a scientific environment.
1understand that / have the right to terminate my membership at any time, which in this case 1must do
in written [orm, to a member of the executive board.
Rio de Janeiro, 23th september 2013
(Place)
(Date)
~
of
/lJ~
~~
Maria de Nazaré Corr
!a Soeiro
_~~e\P~~'()v~~
~ ~y~\o\~~\)t.~?,.'b
~
\JJo'O' ~\OV~fô'S
Please fill in, print and sign this formo It can be sent back as hardcOpr~~~
as a scanned pdf
~.\.
Name André Gustavo Tempone
title(s) MSc, PhD
First name
Academic
Institution: Instituto Adolfo Lutz, Secretary of Health of Sao Paulo
Department: Parasitology and Mycology
Function: Scientific Researcher V
For the latest years our group have been studying plant and marine metabolites as novel prototypes for
drugs against Leishmania and Trypanosoma cruzi parasites with Prof. João HG Lago and Prof Roberto
Berlinck, respectively. Since the beginning of the ResNetNPND, we have started a collaborative work
with Prof. Vitor Ferreira´s group from Rio de Janeiro, Brazil, to study synthetic naphtoquinones, with
contribution of Prof. Thomas Schmidt (University of Munster) and Fernando Costa (University of Sao
Paulo) for the in silico QSAR studies.
Please give full bibliography of all your scientific publications relevant to the field in the years
2011, 2012 and 2013. Please mark those that were co-authored by at least one further member
of ResNet NPND in red (irrespective of whether you made an acknowledgement to ResNet
NPND, or not).
1. Correa DS, Tempone AG, Reimao JQ, et al. Anti-leishmanial and anti-trypanosomal potential
of polygodial isolated from stem barks of Drimys brasiliensis Miers
(Winteraceae). Parasitology Research. Jul 2011;109(1):231-236.
2. De Oliveira A, Mesquita JT, Tempone AG, Lago JHG, Guimaraes EF, Kato MJ. Leishmanicidal
activity of an alkenylphenol from Piper malacophyllum is related to plasma membrane
disruption. Experimental Parasitology. Nov 2012;132(3):383-387.
3. dos Santos RT, Hiramoto LL, Lago JHG, et al. ANTI-TRYPANOSOMAL ACTIVITY OF 1,2,3,4,6PENTA-O-GALLOYL-beta-D-GLUCOSE ISOLATED FROM Plectranthus barbatus Andrews
(Lamiaceae). Quimica Nova. 2012;35(11):2229-2232.
4. Grecco SD, Reimao JQ, Tempone AG, et al. In vitro antileishmanial and antitrypanosomal
activities of flavanones from Baccharis retusa DC. (Asteraceae). Experimental
Parasitology. Feb 2012;130(2):141-145.
5. Grecco SS, Reimao JQ, Tempone AG, et al. Isolation of an antileishmanial and
antitrypanosomal flavanone from the leaves of Baccharis retusa DC.
(Asteraceae). Parasitology Research. Apr 2010;106(5):1245-1248.
6. Jafari R, Najafzadeh N, Sedaghat MM, Patvizi P. Molecular characterization of sandflies and
Leishmania detection in main vector of zoonotic cutaneous leishmaniasis in Abarkouh
district of Yazd province, Iran. Asian Pacific Journal of Tropical Medicine. Oct
2013;6(10):792-797.
7. Morais TR, Romoff P, Favero OA, et al. Anti-malarial, anti-trypanosomal, and antileishmanial activities of jacaranone isolated from Pentacalia desiderabilis (Vell.)
Cuatrec. (Asteraceae). Parasitology Research. Jan 2012;110(1):95-101.
8. Sartorelli P, Santana JS, Guadagnin RC, et al. IN VITRO TRYPANOCIDAL EVALUATION OF
PINANE DERIVATIVES FROM ESSENTIAL OILS OF RIPE FRUITS FROM Schinus
terebinthifolius RADDI (ANACARDIACEAE). Quimica Nova.2012;35(4):743-747.
9. Schmidt TJ, Khalid SA, Romanha AJ, et al. The Potential of Secondary Metabolites from
Plants as Drugs or Leads Against Protozoan Neglected Diseases - Part II. Current
Medicinal Chemistry. May 2012;19(14):2176-2228.
10. Schmidt TJ, Khalid SA, Romanha AJ, et al. The Potential of Secondary Metabolites from
Plants as Drugs or Leads Against Protozoan Neglected Diseases - Part I. Current
Medicinal Chemistry. May 2012;19(14):2128-2175.
with ResNet NPND.
The participation in ResNet NPND allows incorporating the knowledge of different
professionals to our Drug Discovery studies. This include the testing of large NP libraries
isolated from plants of different parts of the world, synthesis of derivatives and in silico studies
to guide lead optimization studies.
It is also important to have a strong network of collaborators to allow the exchange of
students, and consequently exchange of experiences. Finally, ResNetNPND give me the
opportunity to have compromised colleagues from different countries involved in the same
goal, neglected diseases.
Many people get interested in participating in networks to exchange ideas, get publishing
opportunities, get funding opportunities, but…at the moment the global financial crisis
dramatically reduced the research support including the developed countries. Money is needed,
but we have to face the truth, it is scarce at the moment and maybe for the next years it will not
be easy to get it. For those who really want to continue in this network, funding must come from
other sources for the next months/years(???), until we have novel funding opportunities. But to
get funding I do agree that we have to show to agencies a strong and efficient network, with
strong publications, and with well-defined functions and goals.
In my opinion, at least one lead compound should be selected by the team to be:
1- synthesized with large library of derivatives.
2- Optimized based in in silico studies (QSAR, PK/PD). Participation of medicinal chemists
to avoid the synthesis of known mutagenic, toxic compounds.
3- Studied their mechanisms of action.
4- Studied in in vivo experiments.
5- Incorporated in different formulations for drug delivery.
Maybe a WHO member could invited to participate in our Network to recommend us what is
“really needed”, e.g. oral formulations, etc…This could also give us a wide visibility to funding
agencies.
Finally the incorporation of novel researchers for the biological testing area is extremely needed.
____________________________________________________________________
(Place)
Sao Paulo
(Date) 5th October , 2013 (Signature)
Questionnaire for ResNet NPND members’ report To all current members: Please fill in and send back by Oct. 15, 2013 1. Personal information Wrenger Carsten Prof. Dr. Name First name Academic title(s) 2. Affiliation – Institution, Department, Function Institution: Institute of Biomedical Science, University of Sao Paulo Department: Unit for Drug Discovery (UDD), Department of Parasitology Function: Head of UDD 3. Report on activities in and for ResNet NPND since April 2011 Please give full bibliography of all your scientific publications relevant to the field in the years 2011, 2012 and 2013. Please mark those that were co‐authored by at least one further member of ResNet NPND in red (irrespective of whether you made an acknowledgement to ResNet NPND, or not). 4. Publications relevant to the field Wrenger C, Müller IB, Schifferdecker AJ, Jain R, Jordanova R, Groves MR (2011) The N‐terminal residues play an important role in the formation of the Plasmodium falciparum aspartate aminotranserase homodimer. J. Mol. Biol. 405, 956‐971 Begum A, Drebes J, Perbandt M, Wrenger C, Betzel C (2011) Purification, crystallization and preliminary X‐ray diffraction analysis of the thiaminase type II in Staphylococcus aureus. Acta Crystallogr. Sect. F 67, 51‐53 Drebes J, Perbandt M, Wrenger C, Betzel C (2011) Purification, crystallization and preliminary X‐
ray diffraction analysis of ThiM from Staphylococcus aureus. Acta Crystallogr. Sect. F 67, 479‐
481 Vieira LP*, Mantilla BS*, Barisón MJ*, Wrenger C, Silber AM (2011) Trypanosoma cruzi mitochondrion: a source for drug targets against Chagas´ disease. Curr. Pharm. Design 17, 2074‐2099 Wrenger C, Müller IB, Silber AM, Jordanova R, Lamzin VS, Groves MR (2012) Aspartate Aminotransferase ‐ Bridging Carbohydrate and Energy Metabolism in Plasmodium falciparum. Curr. Drug Metabolism 13, 332‐326 Knöckel J, Müller IB, Butzloff S, Bergmann B, Walter RD, Wrenger C (2012) The antioxidative effect of de novo generated vitamin B6 in Plasmodium falciparum validated by protein interference. Biochem. J. Disease 443, 397‐405 Ndjonka D, Bergmann B, Agyare C, Lüersen K, Hensel A, Wrenger C, Liebau E (2012) Screening, combination of plant extracts and activity of pure compound from Phyllanthus muellerianus and Anogeissus leiocarpus against Plasmodium falciparum. Parasitol. Res. 14, 3395‐3439 Wrenger C, Müller IB, Butzloff S, Jordanova R, Lunev S, Groves MR (2012) Crystallization and Preliminary X‐ray Diffraction of Malate Dehydrogenase from Plasmodium falciparum. Acta Crystallogr. Sect. F 68, 659‐662 Butzloff S, Groves MR, Wrenger C#, Müller IB# (2012) Cytometric quantification of singlet oxygen in the human malaria parasite Plasmodium falciparum. Cytometry A 81, 698‐703 Reeksting SB, Müller IB, Burger PB, Burgos ES, Salmon L, Louw AI, Birkholtz LM, Wrenger C (2013) Exploring inhibition of Pdx1, a component of the PLP synthase complex of the human malaria parasite Plasmodium falciparum. Biochem. J. Chem. Biol. 449, 175‐187 “Key Publication” in Global Medical Discovery Ndjonka D*, Rapado LN*, Silber AM, Liebau E, Wrenger C (2013) Natural products as a source for treating neglected parasitic diseases. Int. J. Mol. Sci. 14, 3395‐3439 Ulrich H, Wrenger C (2013) Identification of aptamers as specific binders and modulators of cell‐
surface receptor activity. Methods Mol. Biol. 986, 17‐39 Kronenberger T, Schettert I, Wrenger C (2013) Targeting the vitamin biosynthesis pathway for the treatment of malaria. Future Med. Chem. 5, 769‐779 Chan XW*, Wrenger C*, Stahl K, Müller IB#, Saliba KJ# (2013) Chemical and genetic validation of thiamine utilization as an antimalarial drug target. Nature Commun. 4, 2060 Highlighted in “Malaria Nexus”, Elsevier Pereira CA, Sayé M, Wrenger C, Miranda MR (2013) Metabolite transporters in trypanosomatid parasites: promising therapeutic targets but… how to deal with them? Curr. Med. Chem. [Epub ahead of print] Begum A* Drebes J*, Kikhney A, Müller IB, Perbandt M, Svergun D, Wrenger C#, Betzel C# (2013) Staphylococcus aureus thiaminase II ‐ Oligomerization warrants proteolytic protection against serine proteases. Acta Crystallogr. D Biol. Crystallogr. (in press) Zimbres FM, Tarnok A, Ulrich H#, Wrenger C# (2013) Aptamers ‐ Novel Molecules as Diagnostic Markers in Bacterial and Viral Infections? Biomed. Res. Int. (in press) Drebes J, Künz M, Pereira CA, Betzel C#, Wrenger C# (2013) MRSA Infections: From classical treatment to suicide drugs. Curr. Med. Chem. (in revision) BOOK CHAPTERS: Becker and Selzer „Apicomplexan Parasites ‐ Molecular Approaches toward Targeted Drug Development” WILEY‐VCH Verlag & Co. KGaA (ISBN: 978‐3‐527‐32731‐7); (Chapter 6) Müller IB, Das Gupta R, Lüersen K, Wrenger C and Walter RD (2011) “Polyamines in Apicomplexan Parasites” Becker and Selzer „Apicomplexan Parasites ‐ Molecular Approaches toward Targeted Drug Development” WILEY‐VCH Verlag & Co. KGaA (ISBN: 978‐3‐527‐32731‐7); (Chapter 12) Wrenger C and Müller IB (2011) “Exploiting the Vitamin Metabolism of Apicomplexa as Drug Targets” Izet Kapetanovic "Drug Development" INTECH Publisher (ISBN: 978‐953‐307‐723‐9); (Chapter 16) Wrenger C and Ulrich H (2011) “Drug Discovery by Aptamers in Protozoan Infectious Diseases“ El‐Shemy “Drug Discovery” INTECH Publishers (ISBN: 980‐953‐307‐545‐2); (Chapter 8) Wrenger C, Schettert I and Liebau E (2013) “Oxidative stress in human infectious diseases ‐ present and current knowledge about its druggability“ Hommel and Kremsner “Encyclopedia of Malaria” Springer Verlag (ISBN: 978‐146‐148‐327‐4); (Chapter 17) Müller IB and Wrenger C (2013) “Vitamin Metabolism in Malaria“ 5. Motivation to continue membership Please give a short statement explaining why you wish to continue your membership and cooperation with ResNet NPND. I think as also stated below the network between is very important to link the natural compound chemistry with the analysis of its effect on pathogen proliferation. In this sense this network suits perfectly the needs of all scientists working in the field of human pathogens. Even further since this network operates on a bi‐continental platform the personal as well as intellectual exchange will warrant a high level of synergy between the scientific institutions in South America and Europe. Therefore I would highly appreciate to continue ResNet NPND by being a member of it. 6. Evaluation of ResNet NPND activities, future perspectives and suggestions for improvement Please give a short statement describing your experiences with ResNet NPND, outline how you would imagine ResNet NPND in the future, including constructive suggestions for improvement. To my opinion this network would benefit from an annual meeting which would bring the members working and analyzing natural compounds closer to those members working more on the applied site – molecular and cellular biology of the pathogens. What do you think about extending ResNet NPND to the field of microbiology on pathogenic bacteria or even fungi? 7. Confirmation of commitment, declaration of scientific independence and signature I hereby confirm that I renew my commitment myself to the aims and goals of ResNet NPND and that I wish to continue my membership in ResNet NPND. At the same time I declare, that I am legally authorized to conduct own research projects, coordinate joint research, publish data and work independently in a scientific environment. I understand that I have the right to terminate my membership at any time, which in this case I must do in written form, to a member of the executive board. Sao Paulo, 23/09/2013 ____________________________________________________________________ (Place) (Date) (Signature) Please fill in, print and sign this form. It can be sent back as hardcopy or, preferably, as a scanned pdf document to thomschm@uni‐muenster.de Questionnaire for ResNet NPND members’ report
Name Ferreira
First name Vitor
Academic title(s) PhD
Institution: Universidade Federal Fluminense
Department: Organic Chemistry
Function: Professor of Chemistry
Our research group has explored the interface between organic chemistry and biology. The combination
of these two areas has allowed us to investigate how molecules interact with our synthetic targets that
have been selected. With this, we are continuously developing new synthetic methodologies to produce
new families of substances that can selectively trigger a biological response against viruses, fungi and
bacteria, with isolated enzymes and constitute pharmacological targets.
See below
1. LOURDES G. FERREIRA, MARIA, PINHEIRO, Luiz C. S., SANTOS-FILHO, OSVALDO A., PEÇANHA,
MARTA D. S., SACRAMENTO, CAROLINA Q., MACHADO, VIVIANE, FERREIRA, VITOR F., SOUZA,
THIAGO MORENO L., BOECHAT, Núbia. 2014. Design, synthesis, and antiviral activity of new 1H-1,2,3triazole nucleoside ribavirin analogs In Medicinal Chemistry Research (Print). , v.23, 1501-1511
2. DE SOUZA, MARCOS C, PEDROSA, LEANDRO F, CAZAGRANDE, GÉSSICA S, FERREIRA, VITOR
F., NEVES, MARIA G P M S, CAVALEIRO, JOSÉ A S. 2014. From porphyrin benzylphosphoramidate
conjugates to the catalytic hydrogenation of 5,10,15,20-tetrakis(pentafluorophenyl)porphyrin In Beilstein
Journal of Organic Chemistry. , v.10, 628-633
3. FERREIRA, VITOR F., ROCHA, DAVID R. DA, SILVA, Fernando de C. da. 2014. Green Chemistry,
Sustainable Economy and Quality of Life In Revista Virtual de Química. , v.6, 85
4. REZENDE, CLAUDIA M., SILVA, Fernando de C. da, ROCHA, DAVID R. DA, FERREIRA, VITOR F..
2014. Piperylene Sulfone: A Smart Solvent In Revista Virtual de Química. , v.6, 131-141
5. GONZAGA, DANIEL, SENGER, MARIO ROBERTO, DA SILVA, FERNANDO DE CARVALHO,
FERREIRA, VITOR F., SILVA, FLORIANO PAES. 2014. 1-Phenyl-1H- and 2-phenyl-2H-1,2,3-triazol
derivatives: Design, synthesis and inhibitory effect on alpha-glycosidases In European Journal of
Medicinal Chemistry. , v.74, 461-476
6. Cardoso, Mariana F. C., SILVA, ILLANA M. C. B. DA, SANTOS JÚNIOR, HELVÉCIO M. DOS, ROCHA,
DAVID R., ARAÚJO, ANA JÉRSIA, Pessoa, Claudia, Moraes, Manoel O. de, LETÍCIA V. C., SILVA,
Fernando de C. da, Santos, Wilson C., FERREIRA, VITOR F... 2013. A new approach for the synthesis of
3-substituted cytotoxic nor-beta-lapachones In Journal of the Brazilian Chemical Society , v.24, 12-16
7. SHARMA, ABHINAY, SANTOS, ISABELA O., GAUR, PRATIBHA, FERREIRA, VITOR F., GARCIA,
CELIA R.S., da Rocha, David R.. 2013. Addition of thiols to o-quinone methide: New 2-hydroxy-3phenylsulfanylmethyl[1,4]naphthoquinones and their activity against the human malaria parasite
Plasmodium falciparum (3D7) In European Journal of Medicinal Chemistry. , v.59, 48-53
8. DOMINGOS, THAISA F. S., MOURA, LAURA DE A., CARVALHO, CARLA, Campos, Vinícius R.,
Jordão, Alessandro K., CUNHA, Anna C., FERREIRA, VITOR F.., de Souza, Maria Cecília B. V.,
Sanchez, Eladio F., FULY, ANDRÉ L.. 2013. Antivenom Effects of 1,2,3-Triazoles against Bothrops
jararaca and Lachesis muta Snakes In BioMed Research International. , v.2013, 1-7
9. FERREIRA, FABRICIA DA ROCHA, FERREIRA, SABRINA BAPTISTA, ARAÚJO, ANA JÉRSIA,
MARINHO FILHO, JOSÉ DELANO BARRETO, PESSOA, CLÁUDIA, MORAES, MANOEL O., COSTALOTUFO, LETÍCIA V., MONTENEGRO, RAQUEL CARVALHO, DA SILVA, FERNANDO DE C.,
FERREIRA, V. F., da Silva, F. C., DA COSTA, JOÃO GOMES, DE ABREU, FABIANE CAXICO,
GOULART, MARÍLIA OLIVEIRA FONSECA. 2013. Arylated
alpha- and beta-dihydrofuran
naphthoquinones: Electrochemical parameters, evaluation of antitumor activity and their correlation In
Electrochimica Acta. , v.110, 634-640
10. CUNHA, Anna C., FERREIRA, VITOR F., Jordão, Alessandro K., DE SOUZA, MARIA C. B. V.,
WARDELL, Solange M. S. V., WARDELL, James L., TAN, PEIYU AMELIA, BETTENS, RYAN P. A.,
SETH, SAIKAT KUMAR, TIEKINK, EDWARD R. T.. 2013. Aryl-substituents moderate the nature of
hydrogen bonds, N-H-N versus N-H-O, leading to supramolecular chains in the crystal structures of Narylamino 1,2,3-triazole esters In CrystEngComm (Cambridge. Online). , v.15, 4917
11. FERREIRA, V. F., MOURA, K. C. G., PINTO, M. C. F. R., DA SILVA JÚNIOR, E. N., DA SILVA
JÚNIOR, E. N.. 2013. Aspectos da Obra Científica de Antonio Ventura Pinto: Uma Vida Dedicada ao
Estudo da Reatividade Química de Quinonas Naturais e Sintéticas In Revista Virtual de Química. , v.5,
1022-1047
12. SCHUCK, DESIREE C, FERREIRA, SABRINA B, CRUZ, LAURA N, DA ROCHA, DAVID R,
MORAES, MIRIAM S, NAKABASHI, MYNA, ROSENTHAL, PHILIP J, FERREIRA, VITOR F., GARCIA,
CELIA RS. 2013.
Biological evaluation of hydroxynaphthoquinones as anti-malarials In Malaria Journal (Online). , v.12, 234
13. FERREIRA, VITOR F., SILVA, Fernando de Carvalho da, FERREIRA, P. G.. 2013. CARBOIDRATOS
COMO FONTE DE COMPOSTOS PARA A INDÚSTRIA DE QUÍMICA FINA In Química Nova , v.36, 1514
14. Gomes, Ana T.P.C., Martins, Priscila R. C., ROCHA, DAVID, Neves, M. Graça P. M. S., FERREIRA,
V. F., , Cavaleiro, José A. S., Silva F C. 2013. Consecutive Tandem Cycloaddition Between Nitriles and
Azides: Synthesis of 5-Amino-1H-[1,2,3]-triazoles In Synlett (Stuttgart). , v.24, 41-44
15. MENEZES, JOSÉ C.J.M.D.S., NEVES, M. GRAÇA P.M.S., Cavaleiro, José A.S., BARROS,
CRISTINA, SANTOS, SÉRGIO M., da Silva, Fernando de C., FERREIRA, VITOR F.., Domingues, M.
Rosário M.. 2013. Gas phase reactions of ß-substituted hetero-Diels-Alder adducts of mesotetraphenylporphyrin using tandem mass spectrometry In International Journal of Mass Spectrometry
(Print). , v.343-344, 1-8
16. CORRÊA, ARLENE G., ZUIN, VÂNIA G., FERREIRA, VITOR F.., VAZQUEZ, PATRICIA G.. 2013.
Green chemistry in Brazil In Pure and Applied Chemistry (Print). , v.85, 1
17. SOARES, FABYANA A., SESTI-COSTA, RENATA, DA SILVA, JOÃO SANTANA, de Souza, Maria
Cecília B.V., FERREIRA, VITOR F.., da C. Santos, Fernanda, MONTEIRO, PATRICIA A.U., LEITÃO,
Andrei, MONTANARI, Carlos A.. 2013. Molecular design, synthesis and biological evaluation of 1,4dihydro-4-oxoquinoline ribonucleosides as TcGAPDH inhibitors with trypanocidal activity In Bioorganic &
Medicinal Chemistry Letters (Print). , v.23, 4597
18. DI ROSSO, MARÍA EMILIA, BARREIRO ARCOS, MARÍA LAURA, ELINGOLD, IGAL, STERLE,
HELENA A., Ferreira, Sabrina Baptista, FERREIRA, VITOR F.., GALLEANO, MÓNICA, CREMASCHI,
GRACIELA, DUBIN, MARTA. 2013. Novel o-naphthoquinones induce apoptosis of EL-4 T lymphoma cells
through the increase of reactive oxygen species In Toxicology in Vitro. , v.27, 2094
19. FERREIRA, VITOR F., DA ROCHA, DAVID R, DA SILVA, FERNANDO C, FERREIRA, PATRÍCIA G,
BOECHAT, NÚBIA A, MAGALHÃES, JORGE L. 2013. Novel 1 -1,2,3-, 2 -1,2,3-, 1 -1,2,4- and 4 -1,2,4triazole derivatives: a patent review (2008 - 2011) In Expert Opinion on Therapeutic Patents. , v.23, 319331
20. DE LUCAS, NANCI C., RUIS, CAROLINA P., TEIXEIRA, RODOLFO I., MARÇAL, LUISA L.,
GARDEN, SIMON J., CORRÊA, RODRIGO J., FERREIRA, SABRINA, NETTO-FERREIRA, JOSÉ
CARLOS, FERREIRA, VITOR F.. 2013. Photosensitizing properties of triplet furano and pyrano-1,2naphthoquinones In Journal of Photochemistry and Photobiology. A, Chemistry. , v.276, 16-30
21. GUIMARÃES, TIAGO T., PINTO, MARIA DO CARMO F.R., LANZA, JULIANE S., MELO, MARIA N.,
DO MONTE-NETO, RUBENS L., DE MELO, ISADORA M.M., DIOGO, EMILAY B.T., FERREIRA, VITOR
F., CAMARA, CELSO A., VALENÇA, WAGNER O., DE OLIVEIRA, RONALDO N., FRÉZARD,
FRÉDÉRIC, DA SILVA JÚNIOR, EUFRÂNIO N.. 2013. Potent naphthoquinones against antimonysensitive and -resistant Leishmania parasites: Synthesis of novel alpha- and nor- alpha-lapachone-based
1,2,3-triazoles by copper-catalyzed azide-alkyne cycloaddition In European Journal of Medicinal
Chemistry. , v.63, 523-530
22. GONZAGA, D. T. G., ROCHA, D. R., SILVA, F. C., VITOR F. FERREIRA. 2013. Recent Advances in
the Synthesis of New Antimycobacterial Agents Based on the 1H-1,2,3-Triazoles In Current Topics in
Medicinal Chemistry (Print). , v.13, 2850-2865
23. MAGALHÃES, J.L., QUONIAM, L., FERREIRA, V. F., FERREIRA, P.G., BOECHAT, N.. 2013.
Research on pharmaceuticals patents in times of Big data: a contribution of the Web 2.0 for medicinal
chemistry In Intellectual Properties Rights: Open Access. , v.13, 1-9
24. Reis, M. I. P., Romeiro, G. A., Damasceno, R. N., da Silva, F. C., FERREIRA, V. F., da Silva, F. C..
2013. Síntese e Aplicações de 1,3,5-Triazinanas In Revista Virtual de Química. , v.5, 283-299
25. FERREIRA, VITOR F., LEAL, KATIA Z., LINDGREN, ERIC B., DE OLIVEIRA, MARA R.P., DE
SOUZA, MARIA CELIA B.V., VASCONCELOS, THATYANA R.A., WARDELL, James L., WARDELL,
Solange M.s.v., Yoneda, Julliane D.. 2013. Structural evaluation of three 2-phenylpyrazolo[4,3-c]quinolin3-one monohydrates In Journal of Molecular Structure (Print). , v.1051, 299
26. LAMBERTI, MARÍA JULIA, RUMIE VITTAR, NATALIA BELÉN, de Carvalho da Silva, Fernando,
FERREIRA, VITOR F.rancisco, RIVAROLA, VIVIANA ALICIA. 2013. Synergistic enhancement of
antitumor effect of beta-Lapachone by photodynamic induction of quinone oxidoreductase (NQO1) In
Phytomedicine (Stuttgart). , v.20, 1007-1012
27. DIOGO, EMILAY B.T., DIAS, GLEISTON G., RODRIGUES, BERNARDO L., GUIMARÃES, Tiago
Teixeira, Guimarães, Tiago T., VALENÇA, WAGNER O., CAMARA, CELSO A., DE OLIVEIRA,
RONALDO N., FERREIRA, V. F., DA SILVA, MAURO G., DE PAIVA, YEN GALDINO, Goulart, Marilia
O.F., Menna-Barreto, Rubem F.S., DE CASTRO, SOLANGE L., Da Silva Júnior, Eufrânio N.. 2013.
Synthesis and anti-Trypanosoma cruzi activity of naphthoquinone-containing triazoles: Electrochemical
studies on the effects of the quinoidal moiety In Bioorganic & Medicinal Chemistry (Print). , v.21, 63376348
28. SILVA, BIANCA N. M., SILVA, BÁRBARA V., SILVA, Fernando C., Gonzaga, Daniel T. G.,
FERREIRA, VITOR F.., Pinto, Angelo C.. 2013. Synthesis of Novel Isatin-Type 5'-(4-Alkyl/Aryl-1 -1,2,3triazoles) via 1,3-Dipolar Cycloaddition Reactions In Journal of the Brazilian Chemical Society , v.24, 179183
29. JORDÃO, ALESSANDRO K., NOVAIS, JULIANA, Bruno L.A. Ferreira, Leal, Bruno, ESCOBAR, ANA
C., DOS SANTOS JÚNIOR, HELVÉCIO M., FERREIRA, V. F., Castro, Helena C.. 2013. Synthesis using
microwave irradiation and antibacterial evaluation of new N,O-acetals and N,S-acetals derived from 2amino-1,4-naphthoquinones In European Journal of Medicinal Chemistry. , v.63, 196-201
30. DA COSTA, EMMERSON C. B., AMORIM, RAQUEL, da Silva, Fernando C., ROCHA, DAVID R.,
PAPA, MICHELLE P., DE ARRUDA, LUCIANA B., MOHANA-BORGES, RONALDO, FERREIRA, VITOR
F.., TANURI, AMILCAR, DA COSTA, LUCIANA J., FERREIRA, Sabrina B.. 2013. Synthetic 1,4-Pyran
Naphthoquinones Are Potent Inhibitors of Dengue Virus Replication In Plos One. , v.8, e82504
31. FOREZI, LUANA DA SILVA MAGALHÃES, SILVA, MARCOS MOITREL PEQUENO, SANTOS,
FERNANDA DA COSTA, FERREIRA, V. F., C. SANTOS, FERNANDA, SOUZA, MARIA CECÍLIA
BASTOS VIEIRA DE. 2013. 1,2:5,6-Di- -isopropylidene-3- -methyl- alpha- -allofuranose In Acta
Crystallographica. Section E. , v.69, o1512-o1512
32. MARTINEZ, S. T., MARTINEZ, SABRINA T., Silva, B. V., PINTO, A. C., CHAVES, V. C., SILVA, F. C.,
Pinto, Angelo C., FERREIRA, VITOR F.., SILVA, Fernando de Carvalho da, SILVA, BÁRBARA V.. 2012.
Adição de anilinas à naftoquinona em água e em fase sólida In Química Nova , v.35, 858-860
33. DE PASCUAL, R., DE LOS RIOS, C., ROSA, J. M., CORREA-LEITE, P. E., ARAUJO, K. G. L.,
FERREIRA, V. F., da Rocha, David R., GONZAGA, D. T. G., GARCÍA, A. G., SANTOS, W. C., GANDÍA,
L.. 2012. Augmentation of catecholamine release elicited by an Eugenia punicifolia extract in chromaffin
cells In Revista Brasileira de Farmacognosia , v.22, 1-12
34. da Silva, F. C., Ferreira, S. B., da Rocha, D. R., FERREIRA, V. F.. 2012. Chagas Disease: Challenges
in Developing New Trypanocidal Lead Compounds In Revista Virtual de Química. , v.4, 22-28
35. SENGER, MARIO ROBERTO, GOMES, LUCAS DA COSTA ANDRADE, FERREIRA, Sabrina
Baptista, Kaiser, Carlos Roland, FERREIRA, V. F., KAISER, C. R., SILVA, FLORIANO PAES. 2012.
Kinetics Studies on the Inhibition Mechanism of Pancreatic alpha-Amylase by Glycoconjugated 1H-1,2,3Triazoles: A New Class of Inhibitors with Hypoglycemiant Activity In ChemBioChem (Print). , v.13, n/a-n/a
36. CARNEIRO, PAULA F., DO NASCIMENTO, SAMARA B., PINTO, Antonio V., PINTO, MARIA DO
CARMO F.R., LECHUGA, GUILHERME C., SANTOS, Dilvani O., DOS SANTOS JÚNIOR, HELVÉCIO M.,
Resende, Jackson A.L.C., BOURGUIGNON, Saulo C., FERREIRA, VITOR F... 2012. New oxirane
derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms In Bioorganic
& Medicinal Chemistry (Print). , v.20, 4995-5000
37. QUEIROZ, RAPHAEL F., Jordão, Alessandro K., CUNHA, Anna C., FERREIRA, VITOR F..,
BRIGAGÃO, MAÍSA R.P.L., MALVEZZI, ALBERTO, DO AMARAL, ANTONIA T., AUGUSTO, OHARA.
2012. Nitroxides attenuate carrageenan-induced inflammation in rat paws by reducing neutrophil
infiltration and the resulting myeloperoxidase-mediated damage In Free Radical Biology & Medicine. ,
v.53, 1942-1953
38. Barros, T. G., Zorzanelli, B. C., PINHEIRO, S., de Brito, M. A., Tanuri A., da Costa, E. C.B., MohanaBorges, R. S., RODRIGUES, Carlos Rangel, de Souza, A.M.T., FERREIRA, V. F., Muri, E. M.F.. 2012.
Novel Peptide Mimetics Based on N-protected Amino Acids Derived from Isomannide as Potential
Inhibitors of NS3 Serine Protease of Hepatitis C Virus In Letters in Organic Chemistry. , v.9, 239-249
39. Pinto, Angelo C., SILVA, Fernando de C. da, FERREIRA, VITOR F... 2012. Otto R. Gottlieb e as
conexões com o Brasil de Ernest Wenkert In Química Nova , v.35, 2317-2322
40. FARO, L. V., FARO, L.V., ALMEIDA, J. M., CIRNE-SANTOS, C., GIONCO, V. A., CASTELLOBRANCO, L. R., Oliveira, I. B., BARBOSA, J. E., FERREIRA, V. F., CUNHA, A. C., SOUZA, M. C.,
FRUGULHETTI, I. C. P. P., SOUZA, M. C. B. V.. 2012. Oxoquinoline acyclonucleoside phosphonate
analogues as a new class of specific inhibitors of human immunodeficiency virus type 1 In Bioorganic &
Medicinal Chemistry Letters (Print). , v.22, 5055-5058
41. da Silva, Fernando de C., JORDÃO, Alessandro Kapel, ROCHA, D. R., Ferreira, S. B., CUNHA, Anna
C, FERREIRA, V. F.. 2012. Recent Advances on the Synthesis of Heterocycles from Diazo Compounds In
Current Organic Chemistry. , v.16, 224-251
42. Luiz C. S. Pinheiro,, BORGES, J. C., dos Santos, M. C., FERREIRA, V. F., BERNARDINO, Alice M.
R., Tonioni, R., Sathler, P. C., CASTRO, Helena C., SANTOS, Dilvani O., Nascimento, S. B.,
BOURGUIGNON, Saulo C., Cabral, L., RODRIGUES, Carlos R.. 2012. Searching for new antileishmanial
lead drug candidates: Synthesis, biological and theoretical evaluations of promising thieno[2,3-b] pyridine
derivatives In Journal of Microbiology and Antimicrobials. , v.4, 32-39
43. Campos, Vinicius R., SANTOS, EVELYNE A. DOS,
DE SOUZA, MARIA C. B. V., Costa-Lotufo, Letícia V.,
Jordão, Alessandro K., Pinto, Angelo C., RESENDE,
Synthesis of carbohydrate-based naphthoquinones and
anticancer agents In RSC ADV. , v.2, 11438
FERREIRA, VITOR F.., Montenegro, Raquel C.,
de Moraes, Manoel O., REGUFE, ANNA K. P.,
JACKSON A. L. C., CUNHA, Anna C.. 2012.
their substituted phenylhydrazono derivatives as
44. da Rocha, David R., Santos, Wilson C., Lima, Emerson S., FERREIRA, V. F.. 2012. Synthesis of
1,2,3-triazole glycoconjugates as inhibitors of --glucosidases In Carbohydrate Research (Chicago, Ill..
Print). , v.350, 14-19
45. Jordão, Alessandro K., FERREIRA, VITOR F.., CUNHA, Anna C., WARDELL, James L., WARDELL,
Solange M. S. V., TIEKINK, EDWARD R. T.. 2012. The differing influence of halides upon supramolecular
aggregation through C-X-; interactions in the crystal structures of (5-methyl-1-(4-X-arylamino)-1H-1,2,3triazol-4-yl)methanol derivatives, X = H, F and Cl In CrystEngComm (Cambridge. Online). , v.14, 6534
46. SCHMIDT, J. T., KHALID, A. S., ROMANHA, J. A., ALVES, M. T., BIAVATTI, M. W., BRUN, R.,
COSTA, F. B., CASTRO, S. L., FERREIRA, V. F., LACERDA, M., LAGO, J. H. G., LEON, L., AMORIN, R.
C. N., NIEHUES, M., OGUNGBE, I. V., POHLIT, M. A., SCOTTI, M. T., SETZER, W. N., SOEIRO, M. N.,
STEINDEL, M., TEMPONE, A. G.. 2012. The Potential of Secondary Metabolites from Plants as Drugs or
Leads Against Protozoan Neglected Diseases - Part I In Current Medicinal Chemistry. , v.19, 2175-2184
47. Schmidt, T.J., Khalid, S.A., Romanha, A.J., Alves, T.M.A., Biavatti, M.W., Brun, R., Da Costa, F.B., de
Castro, S.L., FERREIRA, V. F., de Lacerda, M.V.G., Lago, J.H.G., Leon, L.L., Lopes, N.P., das Neves
Amorim, R.C., Niehues, M., Ogungbe, I.V., Pohlit, A.M., Scotti, M.T., Setzer, W.N., Soeiro, M. de N.C.,
Steindel, M., Tempone, A.G.. 2012. The Potential of Secondary Metabolites from Plants as Drugs or
Leads Against Protozoan Neglected Diseases - Part II In Current Medicinal Chemistry. , v.19, 2176-2228
48. C. SANTOS, FERNANDA, CASTRO, Helena C., LOURENÇO, Maria Cristina S., Abreu, Paula A.,
Batalha, Pedro N., CUNHA, Anna C., CARVALHO, GUILHERME S. L., RODRIGUES, Carlos R.,
Medeiros, Cid A., SOUZA, SIMONE D., FERREIRA, VITOR F.., SOUZA, MARIA C. B. V.. 2012.
Tuberculosis: Finding a New Potential Antimycobacterium Derivative in a Aldehyde-ArylhydrazoneOxoquinoline Series In Current Microbiology. , v.65, 1-8
49. BOECHAT, Nubia, FERREIRA, VITOR F.., FERREIRA, Sabrina B., FERREIRA, Maria de Lourdes G.,
da Silva, Fernando de C., Bastos, Monica M., Costa, Marilia dos S., Lourenc-o, Maria Cristina S., Pinto,
Angelo C., Krettli, Antoniana U., Aguiar, Anna Caroline, Teixeira, Brunno M., da Silva, Nathalia V.,
Martins, Priscila R. C., Bezerra, Flavio Augusto F. M., Camilo, Ane Louise S., da Silva, Gerson P., Costa,
Carolina C. P.. 2011. Novel 1,2,3-Triazole Derivatives for Use against
Mycobacterium tuberculosis
H37Rv (ATCC 27294) Strain In Journal of Medicinal Chemistry. , v.54, 5988-5999
50. Ferreira, S. B., ROCHA, D. R., CARNEIRO, J. W. M., Santos W. C., FERREIRA, V. F.. 2011. A New
Method to Prepare 3-Alkyl-2-hydroxy-1,4-naphthoquinones: Synthesis of Lapachol and Phthiocol In
Synlett (Stuttgart). , v.000, 1551-1554
51. Ana T. P. C. Gomes, Neves, M. G. M. S., Tomé, A. C., Artur M. S. Silva, SOUZA, M. C. B. V.,
FERREIRA, VITOR F.., Cavaleiro, J.A.S.. 2011. Catalytic carbene insertion into an aminoporphyrin and
formation of a new chiral supramolecular porphyrin system In Tetrahedron Letters. , v.52, 4741-4744
52. Yoneda, Julliane D., Velloso, Marcia Helena R., Leal, Kátia Z., Azeredo, Rodrigo B. de V., Sugiura,
Makiko, Albuquerque, Magaly G., Santos, Fernanda da C., SOUZA, Maria Cecília B.v. de, CUNHA, Anna
Claudia, SEIDL, Peter R., FERREIRA, V. F.. 2011. Conformational analysis of a quinolonic ribonucleoside
with anti-HSV-1 activity In Journal of Molecular Structure (Print). , v.985, 1-4
53. Marcelo I. P. Reis, da Silva, Fernando C., Romeiro, Gilberto A., FERREIRA, VITOR F... 2011.
Deposição Mineral em Superfícies: Problemas e Oportunidades na Indústria do Petróleo In Revista Virtual
de Química. , v.3, 2-13
54. Jordão, Alessandro K., Camargos Resende, Jackson A. L., ANNA, C., Lorenzo Sorace, FERREIRA,
VITOR F.., Miguel A. Novak, Claudio Sangregorio, Vaz, Maria G.F.. 2011. Determination of the relevant
magnetic interactions in low-dimensional molecular materials: the fundamental role of single crystal high
frequency EPR In Dalton Transactions (2003. Print). , v.40, 10843-10850
55. Lourenço, André L., Paula A. Abreu, Bruno Leal, Silva Júnior E. N., PINTO, Antonio V., Pinto, M. C. F.
R>, Pinto, M. C. F. R>, SOUZA, Alessandra M. T., Novais, J. S., Paiva, M. B., CABRAL, L. M.,
RODRIGUES, Carlos R., FERREIRA, V. F., CASTRO, Helena C.. 2011. Identification of Nor-betaLapachone Derivatives as Potential Antibacterial Compounds against Enterococcus faecalis Clinical Strain
In Current Microbiology (Print). , v.62, 684-689
56. Pires, Sónia M. G., Paula, Rodrigo De, Simões, Mário M. Q., Silva, Artur M. S., Domingues, M.
Rosário M., Santos, Isabel C. M. S., Vargas, Maria D., Ferreira, Vítor F., Neves, M. Graça P. M. S.,
Cavaleiro, José A. S., FERREIRA, V. F.. 2011. Novel biomimetic oxidation of lapachol with H2O2
catalysed by a manganese(III) porphyrin complex In RSC Advances: an international journal to further the
chemical sciences. , v.1, 1195-1199
57. BOECHAT, Nubia, FERREIRA, V. F., FERREIRA, S. B., COSTA, M. S., SILVA, F. C., LOURENÇO,
Maria Crsitina S, PINTO, Angelo C., FERREIRA, M. L. G., BASTOS, M. M., KRETTLI, A. U., AGUIAR, A.
C., TEIXEIRA, B. M., da SILVA, N. V., MARTINS, P. R., BEZERRA, F. A. F., CAMILO, A. L. S., SILVA, G.
P., COSTA, C. C. P.. 2011. Novel 1,2,3-Triazole Derivates for Use against Mycobacterium tuberculosis
H37Rv (ATCC27294) Strain In Journal of Medicinal Chemistry v.54, 5988-5999
58. ABREU, P. A., Santos, F. C. , CASTRO, H., SOUZA, T., RIBEIRO, C. P., BARBOSA, J. E. F., Cunha,
A.C, FERREIRA, V. F., Paixão, I.C.P. 2011. Oxoquinoline derivatives: Identification and structure-activity
relationship (SAR) analysis of new anti-HSV-1 agents. Current Microbiology, v.62, 1349-54
59. Leandro F. Pedrosa, Marcos C. de Souza, Maria A. F. Faustino, Neves, M. G. M. S., Artur M. S. Silva,
Tomé, A. C., FERREIRA, V. F., Cavaleiro, J.A.S.. 2011. Porphyrin]Phosphoramidate Conjugates:
Synthesis, Photostability and Singlet Oxygen Generation In Australian Journal of Chemistry (Print). , v.64,
939-944
60. Menezes, J.C.J.M.D.S., Gomes, A.T.P.C., Silva, A.M.S., Faustino, M.A.F., Neves, M. G. M. S., Tomé,
A. C., SILVA, F. C., FERREIRA, V. F.. 2011. Reaction of beta-Vinyl-meso-tetraphenylporphyrin with orthoQuinone Methides In Synlett (Stuttgart). , v.000, 1841-1846
61. Reis, R.R., Azevedo, E.C., de Souza, Maria C.B.V., FERREIRA, V. F., Araújo, A. J., Pessoa, C.,
Costa-Lotufo, L. V., MORAES, M. O., Filho, J.D.B.M., de Souza, A.M.T., de Carvalho, N.C., CASTRO,
Helena C., RODRIGUES, Carlos R., Vasconcelos, T.R.A.. 2011.
Synthesis and anticancer activities of some novel 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-pyrazolo[4,3c]quinolin-3(5H)-ones In European Journal of Medicinal Chemistry. , v.46, 1448-1452
62. Jordão, Alessandro K., FERREIRA, V. F., SOUZA, Thiago M. L., Faria, G.G.S., Machado, V.,
Abrantes, J.L., SOUZA, Maria C. B. V. de, ANNA, C.. 2011. Synthesis and anti-HSV-1 activity of new
1,2,3-triazole derivatives In Bioorganic & Medicinal Chemistry (Print). , v.19, 1860-1865
63. Ferreira, S. B., Salomão, K., SILVA, F. C., PINTO, A. V., Kaiser. C. R., PINTO, A. C., FERREIRA, V.
F., De CASTRO, S. L.. 2011. Synthesis and anti-Trypanosoma cruzi activity of beta-lapachone analogues
In European Journal of Medicinal Chemistry. , v.46, 3071-3077
64. Gomes, Ana T.P.C., CUNHA, Anna C., Domingues, Maria do Rosário M., Neves, Maria G.P.M.S.,
Tomé, Augusto C., Silva, Artur M.S., Santos, Fernanda da C., Souza, Maria C.B.V., FERREIRA, VITOR
F.., Cavaleiro, José A.S., FERREIRA, V. F.. 2011. Synthesis and characterization of new porphyrin/4quinolone conjugates In Tetrahedron (Oxford. Print). , v.67, 7336-7342
65. Jordão, Alessandro K., Sathler, Plínio C., FERREIRA, VITOR F.., Campos, Vinícius R., de Souza,
Maria C.B.V., CASTRO, Helena C., Lannes, Andressa, Lourenco, André, RODRIGUES, Carlos R., Bello,
Murilo L., Lourenco, Maria C.S., Carvalho, Guilherme S.L., Almeida, Maria C.B., CUNHA, Anna C.,
FERREIRA, V. F.. 2011. Synthesis, antitubercular activity, and SAR study of N-substituted-phenylamino5-methyl-1H-1,2,3-triazole-4-carbohydrazides In Bioorganic & Medicinal Chemistry (Print). , v.19, 56055611
66. Souza, Denise A., Moreno, Yanko, Ponzio, Eduardo A., Resende, Jackson A.L.C., Jordão, Alessandro
K., CUNHA, Anna C., FERREIRA, VITOR F.., Novak, Miguel A., Vaz, Maria G.F., FERREIRA, V. F.. 2011.
Synthesis, crystal structure, magnetism and electrochemical properties of two copper(II)
furoyltrifluoroacetonate complexes with nitroxide radical In Inorganica Chimica Acta (Testo stampato). ,
v.370, 469-473
67. Ferreira, S. B., Gonzaga, Daniel T. G., da Silva, Fernando C., Araujo K. G. L., FERREIRA, V. F..
2011. Synthesis of New o-Quinone Methides from Beta-Lapachone Analogues In Synlett (Stuttgart). ,
v.000, 1623-11625
68. Jordão, Alessandro K., FERREIRA, V. F., PINTO, A. C., SOUZA, M. C. B. V., ANNA, C.. 2011.
Synthesis of New 2-Aminocarbohydrate-1,4-Naphthoquinone Derivatives Promoted by Ultrasonic
Irradiation In Journal of the Brazilian Chemical Society , v.22, 187-193
69. Rodrigues da Rocha, David, Gusmão de Souza, Ana Carolina, Camargos Resende, Jackson A. L., da
Costa Santos, Wilson, Alves dos Santos, Evelyne, Pessoa, Cláudia, Odorico de Moraes, Manoel, CostaLotufo, Letícia V., Carvalho Montenegro, Raquel, FERREIRA, VITOR F... 2011. Synthesis of new 9hydroxy-alfa- and 7-hydroxy-Beta-pyran naphthoquinones and cytotoxicity against cancer cell lines In
Organic & Biomolecular Chemistry. , v.9, 4315-4322
70. BOURGUIGNON, Saulo C., CAVALCANTI, Danielle F.b., de Souza, Alessandra M.T., CASTRO,
Helena C., RODRIGUES, Carlos R., Albuquerque, Magaly G., SANTOS, Dilvani O., da Silva, Gabriel
Gomes, da Silva, Fernando C., FERREIRA, VITOR F... 2011. Trypanosoma cruzi: Insights into
naphthoquinone effects on growth and proteinase activity In Experimental Parasitology. , v.127, 160-166
71. Marcelo I. P. Reis, Mendes, M. T., da Silva, Fernando de C., FERREIRA, V. F.. 2011. deltaGliconolactona em Síntese Orgânica In Revista Virtual de Química. , v.3, 247-274
with ResNet NPND.
My motivation to stay on the network is related to the possibility of new national and
international scientific collaborations.
My participation in the ResNet NPND network with collaborative work was reduced. I have
worked with Dr. Solange Castro, who was established previous to the network, Dr. André
Tempone that started just before my entrance in the network but is consolidating and Prof.
Thomas Schmidt that began after entry into the network.
____________________________________________________________________
(Place)
(Date)
(Signature)
Questionnaire for ResNet NPND members’ report To all current members: Please fill in and send back by Oct. 15, 2013 1. Personal information Steindel Mário Dr Name First name Academic title(s) 2. Affiliation – Institution, Department, Function Institution: Universidade Federal de Santa Catarina Department: Microbiologia, Imunologia e Parasitologia Function: Professor 3. Report on activities in and for ResNet NPND since April 2011 Please give a short description on your activities within ResNet NPND (anything you did to advance joint research with or among ResNet members, to promote the network). 1-‐ A collaborative project with Dr Alvaro Jose Romanha and Dr. Tania Maria Almeida Alves: Screening plant and fungi extracts against Chagas disease; 2-‐ A collaborative project with Dr Alvaro Jose Romanha and Dr. Tania Maria Almeida Alves: Hits from Natural P roducts for development of new drugs against leishmaniasis, Chagas disease, cancer, dengue and influenza 4. Publications relevant to the field Please give full bibliography of all your scientific publications relevant to the field in the years 2011, 2012 and 2013. Please mark those that were co-‐authored by at least one further member of ResNet NPND in red (irrespective of whether you made an acknowledgement to ResNet NPND, or not). 1. Braga, SFP; Alves, VP; Ferreira, RS; Fradico, JRB; Lage, PS; Duarte, MC; Ribeiro, TG; Júnior,
Policarpo AS; Romanha, AJ.; Tonini, ML. ; Steindel, M; Coelho, EF. ; de Oliveira, RB. Synthesis and
evaluation of the antiparasitic activity of bis-(arylmethylidene) cycloalkanones. European Journal of
Medicinal Chemistry, v. 71, p. 282-289, 2014.
2. Monga, V; Goyal, K; Steindel, M; Malhotra, M; Rajani, DP. ; Rajani, SD. Synthesis and evaluation of
new chalcones, derived pyrazoline and cyclohexenone derivatives as potent antimicrobial, antitubercular
and antileishmanial agents. Medicinal Chemistry Research (Print), v. 23, p. 2019-2032, 2014.
3. Bianco, E; de Oliveira, S; Rigotto, C; Tonini, ML; da Rosa Guimarães, T; Bittencourt, F; Gouvêa, L;
Aresi, C; De Almeida, M; Moritz, M; Martins, C; Scherner, F; Carraro, J; Horta, P; Reginatto, F;
Steindel, M; Simões, CMO; Schenkel, E. Anti-Infective Potential of Marine Invertebrates and Seaweeds
from the Brazilian Coast. Molecules (Basel. Online), v. 18, p. 5761-5778, 2013.
4. Yamanaka, CN; Giordani, RB; Rezende, CO; Eger, I; Kessler, RL; Tonini, ML; de Moraes, MH;
Araújo, DP; Zuanazzi, JA; de Almeida, MV; Steindel, M. Assessment of Leishmanicidal and
Trypanocidal Activities of Aliphatic Diamine Derivatives. Chemical Biology & Drug Design, v. 82, p.
697-704, 2013.
5. Santos TG.; Rebelo, RA; Dalmarco E.M; Guedes A; Gasper AL; Schmit AP; Nunes, RK; Steindel, M.
Composição química e avaliação da atividade antimicrobiana do óleo essencial das folhas de Piper
malacophyllum (C. Presl.) C. DC. Química Nova, v. 35, p. 477-481, 2012.
6. Rebelo, RA; Vannini B; Santos TG; Purnhagen LRP; Butzke ETB; Kempt M; Begnini, IM; Dalmarco
EM; Bela Cruz A; Schmit AP; Cruz RCB; Yamanaka CN; Steindel, M. Chemical characterization and
antimicrobial evaluation of the essential oils from D.C. and D.C. (Asteraceae). The Journal of Essential
Oil Research, v. 24, p. 547-554, 2012.
7. Schmidt TJ; Khalid SA; Romanha AJ ; Alves TM ; Biavatti MW ; Brun R ; Da Costa FB ; De Castro
SL ; Ferreira VF ; De Lacerda MV ; Lago JH ; Leon LL ; Lopes NP ; Das Neves Amorim RC ; Niehues
M ; Ogungbe IV ; Polhlit AM ; Scotti MT ; Setzer WN ; Soeiro MD ; Steindel, Mario ; Tempone AG .
The Potential of Secondary Metabolites from Plants as Drugs or Leads Against Protozoan Neglected
Diseases - Part I.. Current Medicinal Chemistry, v. 19, p. 2128-2175, 2012.
8. Schmidt TJ; Khalid SA ; Romanha AJ; Alves TM; Biavatti MW ; Brun R ; Da Costa FB ; de Castro SL
; Ferreira VF ; de Lacerda MV ; Lago JH ; Leon LL ; Lopes NP ; das Neves Amorim RC ; Niehues M ;
Ogungbe IV ; Polhlit AM ; Scotti MT ; Setzer WN ; Soeiro MD ; Steindel, Mario ; Tempone AG . The
Potential of Secondary Metabolites from Plants as Drugs or Leads Against Protozoan Neglected Diseases
- Part II.. Current Medicinal Chemistry, v. 19, p. 2176-2228, 2012.
9. Almeida, MRR; Tonini, ML; Guimaraes, TR; Bianco, EM; Moritz, MIG; Oliveira, SQ; Cabrera, GM;
Palermo, JA; Steindel, M; Schenckel, EP; Reginatto, F. Anti-Infective Pregnane steroid from octocoral
Carijoa riisei collected in south Brazil. Acta Farmaceutica Bonaerense, v. 31, p. 1489-1495, 2012.
10. Mattos, CB; Deponti, VB; Barreto, F; Simões, CMO; Andrighetti-Fröhner, CR; Nunes, RJ; Steindel,
M; Teixeira, HF; Koester, LS. Development of a stability-indicating LC method for determination of a
synthetic chalcone derivative in a nanoemulsion dosage form and identification of the main
photodegradation product by LC MS. Journal of Pharmaceutical and Biomedical Analysis (Print), v. 70,
p. 652-656, 2012.
11. Bello, ML; Chiaradia, LD; Dias, LRS; Pacheco, LK; Stumpf, TR; Mascarello, A; Steindel, M; Yunes,
RA; Castro, HC; Nunes, RJ; Rodrigues, CR. Trimethoxy-Chalcone derivatives inhibit growth of
Leishmania braziliensis: Synthesis, Biological Evaluation, Molecular Modeling and Structure Activity
Relationship (SAR). Bioorganic & Medicinal Chemistry (Print), v. 19, p. 5046-5052, 2011.
5. Motivation to continue membership Please give a short statement explaining why you wish to continue your membership and cooperation with ResNet NPND. I wish to continue my membership in ResNetNPND because I strongly believe that with joint efforts we can achieve our purpose with success. 6. Evaluation of ResNet NPND activities, future perspectives and suggestions for improvement Please give a short statement describing your experiences with ResNet NPND, outline how you would imagine ResNet NPND in the future, including constructive suggestions for improvement. 1-‐ First of all we need efforts to strengthen cooperation between the network members. I hope that Rio meeting will be a excellent opportunity; 2-‐ Improvement of new strategies for financial support 3-‐ Bioassays standardization. 7. Confirmation of commitment, declaration of scientific independence and signature I hereby confirm that I renew my commitment myself to the aims and goals of ResNet NPND and that I wish to continue my membership in ResNet NPND. At the same time I declare, that I am legally authorized to conduct own research projects, coordinate joint research, publish data and work independently in a scientific environment. I understand that I have the right to terminate my membership at any time, which in this case I must do in written form, to a member of the executive board. Florianopolis 31/03/2014 (Place) (Date) (Signature) Please fill in, print and sign this form. It can be sent back as hardcopy or, preferably, as a scanned pdf document to thomschm@uni-‐muenster.de New members‘ applications (Oct. 2013 – Feb 2014)
Applicotion for membership in ResNet NPND
(Ihis document is occomponied
by q document with some formol
rules ond
explonotions obout the network os well qs o copy of the ResNet NPND Memorondum of
Commitment signed py the founding members in
corefully <:nd then fill in the following form).
20.l
l, Pleose reod ihis docunrent
Pleose type requested informotions
l.
Personolinformotion
Adeleke
First nome
ADEBAJO
Surnome
2. Affiliotion - lnstitution,
Prof. Dr. Phqrm.
Acodemic title(s)
nt, Function
lnstitution: FACULTY OF PHARMACY. OBAFEMI AWOLOWO UNIVERSITY,
ILE-IFE.
NIGERIA.
Deportment: DEPARTMENT OF PHARMACOGNOSY
Function: Former: Heqd of Dept., Current: Lecturer/Reseorcher, Editor-in-Chief,
lfe Journol of Science & Technology, Deputy-Choirmon, University
Ceremoniols Committee, Member, University Reseorch Committee.
3.
Stotement of motivotion
Pleose type o slolemenf exploining your motivotion toioin ResNef NPND {mox.
1000
choroclers, inctu ding spoces/.
My visit to Prof. Schmidt's lob in 2005 ond the ensuing publicotions convinced
me to seek colloborotion with him. This wos with the oim of mqintoning the
good quolity of my publicotions using the spectrqlfqcilities in WWU, Muenster os
well os the HPLC profiling in his loborotory to determine the percenioge of
octive constituents in the qctive froctions. Since he is olso o member of ResNet
NPND, I qm sure thot if ljoin this network, lwould be oble to enjoy these
focilities. Lostly, I hope to benefit from members of the neiwork thqt hqve
fqcilities f or in vifro qnti-moloriol qnd onti-kyponocidql testing thot could
complement the in vivo ossoys used in monitoring octivity-directed purificotions
thqi resulted in our isoloted compounds. Low yields hqve olwoys been the mqin
problem of identifying the octive onti-infective qnd onti-diobeiic constituents.
Poge
I of4
4.
Expertise ond experience in the field
P/eose give o shorf description of your scientific bockground, experiise ond experience
in lhe field of noturolproducts, neg/ecfed diseoses or, optimolly, both (mox. 1000
choroclers, inclu ding spoces/.
A phormocist with lfe Ph.D. (Phormocognosy) degree. Thesis wos on structurql
elucidotion of l5 corbozole qlkqloids, 23 furocoumorins ond four corbozole
qlkoloid derivoiives, including bicyclomohonimbiline, q novel bicyclocorbozole.
Ph.D. work wos storied in Muensier on Sri Lonkon Murraya koenigii ond
completed on thot growing in Nigerio. Reseorch focus is on qnti-irypqnocidol,
onti-trichomonol ond onti-plosmodiol (onti-infective) ossoys of extrqcts,
froctions qnd constituents of plonis used os such, ethnomedicolly. The first 2
were with other biologists. Active chromotogrophic froctions qnd constituents
of folkloricolly used qnti-diobetic plonts were identified. Properties for selection
of potentiol Nigerion plont lorvicides were determined using Aedes oegypti,
vectors of Chogos ond Dengue fevers. Currently working on identifying octive
constituents of plonts with both onti-diobetic qnd qnti-infective properties to
justify their ethnomedicol cloims ond exploin rotionole for their use.
5.
Scientific methods used
Pleose give o shorl description of fhe scienfific melhods ovoiloble in your loboratory,
wilh specio/emphosis on speciolized non-stondord methodologies possibly nol
ovoilqble to mony olhers in the nelwork (mox. 1000 chorocfers, including spoces/.
ln vivo onti-plosmodiol ond onti-pyretic testing, using prophyloctic, curotive ond
chemosuppression models, for individuol herbql drugs os well os their
combinotions.
ln collqborotion with q biologist, in vivo onti-tryponocidol testing of herbol
drugs.
6.
Publicotions in the field
P/eose give fullbibliogrophy of your 5 mosf imporfonf scientific publicqtions
relevonf to the field.
l. A.C. Adebojo, M.D. Ayoolo, S.A. Odediron, A.J. Alodesonmi, T.J. Schmidt
qnd E.J. Verspohl (20.l3). Evoluotion of ethnomedicol cloims lll:Antihyperglycoemic octivities of Gongronemo lotifolium root ond stem.
Jovrnolof Diobefes. 5, 336-343. DOI: l0.l I I 1/1753-0407.12019.
2. A.C. Adebojo, S:A. Odediron, C.M. Nneji, E.O. lwolewo, G.M. Rukungo, A.J.
Alqdesonmi, J.W. Gqthirwq, O.G. Ademowo, T.A. Qlugbode, T.J. Schmidt
ond E.J. Verspohl (2013). Evoluotion of eihnomedicql cloims ll: Antimqloriol
ociivities of Gongronemo lotifolium root ond stem. Journalof Herbs, Spices
ond Medicinol P/onfs. I 9, 97 -1 I 8. DOI: I 0. I 080/ I 049 647 5.2012734012.
Poge 2 of 4
give fvll bibliogrophy of your 5 most importont scieniific PUbticotions relevonl to
lhe field.
A.C. Adebojo, F.G. Fomuyiwo, J.D. John, E.S. ldem ond A.o. Adeoye.
,;;*
3.
4.
plonts ogoinst Aedes oegypti'
t21l2).nctivitLs of some'Xtigerion medicinol
bhin.se Medicine, 3(3), I 5l-l 56. doi: I 0'4236/cm'2012'
A.C. Adebojo, E.o. lwolewq, E.M. Obuotor" G.F. lbikunle, N.O. Omisore,
c.o. Adewunmi, o o. oboporusi, M. Kloes, G.E. Adetogun,T.J. Schmidt ond
the extroct ond some
E. J. Verspohl. (2009). Phormqcologicol properties of
ontiisoloted compounds of Clousenq Lnsium stem bqrk: Anti-trichomonol,
qntioxidont
Journal
effects.
diobetic, qnti-inflommotory, hepotoprotective
.l9.
of EthnoPhormacologY, 122,.l0
5.
-
Adewunmi, C.Q., Agbedohunsi, J.M', Adebojo, A'C" Alqdesqnmi' A'J"
of
Murphy, N., qnd WdnOo, J. (200,l). Eihno-veterinory medicine: Screening
Nigerion medicinql plonts for tryponocidql properties. Journolof
EthnopharmocologY, 77, 19 - 24.
Pleose lisl
ocfive cooperotions wifh relevonce to the field' Pvt speciol emphosis on
NPND'
exisling cooperolions wifh scienfisfs who ore olreody members of ResNel
piof. Dr. TJ Schmidt for spectrol onolysis ond HPLC profiling.
Prof. Dr. EJ Verspohl for in vitro insulin testing'
in vitro qntiDrs. G.M. Rukungo ond J.w. Gothirwo, KEMRI, Kenyo for
plqsmodiol testing to confir:m in vivo done in our loborotory.
l.
2.
3.
totions
ond ocfive
Pleose give o short outlin e on (o) whol you expecf from o membership
you (mox.
from
expecl
con
NPND
ResNef
contribution to ResNet NPND ona b) whol
500 choroc lers, including spcrcesJ.
o.
l. Complete (NMR, MS, etc) spectrol onolyses of our isoloted compounds
for publicotion in creditoble journols
2. HPLC profiling of qctive extrqcts & frqctions for publicotion ond
registrotion os drug in Nigerio.
3. ln vitro ossoys to confirm in vivo qssqys done in our lob.
4. Shori reseqrch fellowships to lqbs of I & 2 obove'
b.
I. End point reseorch publicotions.
2. ln vivo ossqys listed under 5 qbove.
in estoblishing relotionship
3. lf proven, ResNetNpND would olso toke credit
qctivities.
between qnti-infective qnd onti-diqbetic
Poge 3 of 4
9.
Comrnitment
P/eose give
o short ovfline on whot ResNel NPND con expect from you in case your
opplicotion is occepfed; pleose o/so moke on esfimqte on lhe imporlonce of wokin
fhrs field for yovr fofo/ scienf ific work /e.g. rn % of your tofol worklood or output) (mox.
500 choracters, inc/udlng spoces/.
Absolute loyolty.
Offer to do the in vivo tests listed obove.
Together with other members of the Network, publicoiion of end product
popers.
65% of my totol workloqd would be dedicoted to the ResNet NPND.
l.
2.
3.
I0. Declqrqtion of scientific independence ond sisnoture
I hereby confirm this opplicotion with my legolsignofure.
At the sorne time ldec/ore, thot tqm tegatly outhorized to conduct own reseorch
proiecfs, coordinatejoini reseorch, publish doto ond workindependently in o scieniific
environmenf. I o/so declore thot I commit myself to lhe oims ond goo/s of ResNel NPND.
/ underslond thot I hove the right to terminate my membershp at ony time, which in fhis
cose / must do in writlen form, to o member of the execuliye boord.
Pleqse fillin, print qnd sign this form. lt con be sent bock qs hardcopy or, preferobly, qs o
sconned pdf document to thomschm@uni-muensier.de
Poge 4 of 4
Application for membership in ResNet NPND (This questionnaire is accompanied by a document with some formal rules and explanations about the network as well as a copy of the ResNet NPND Memorandum of Commitment signed by the founding members in 2011. Please read this document carefully and then fill in the following form). Please type requested informations 1. Personal information Name : Maes Cos Delputte First name: Louis Academic title(s) PhD, professor Paul PhD, professor Peter PhD, professor 2. Affiliation – Institution, Department, Function Institution: Laboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp Department: Faculty of Pharmaceutical, Biomedical and Veterinary Sciences Function: Professor 3. Statement of motivation Please type a statement explaining your motivation to join ResNet NPND (max. 1000 characters, including spaces). Our research group LMPH is seeking for new molecules with clinically relevant biological activities for further in depth evaluation in joint projects. We can contribute to unravel the mechanism-‐of-‐action/pharmacodynamics and to strengthen proof-‐of-‐concept of these bioactive molecules. 4. Expertise and experience in the field Please give a short description of your scientific background, expertise and experience in the field of natural products, neglected diseases or, optimally, both (max. 1000 characters, including spaces). LMPH is a research group of the University of Antwerp with 26 members. LMPH is run by Prof. Louis Maes, Prof. Paul Cos and Prof. Peter Delputte and currently comprises 13 PhD students, 2 post-‐doctoral researchers and a team of laboratory technicians. Strong fundamental and applied expertise has been gained in leishmaniasis, with a particular focus on drug discovery, resistance evaluation, cell-‐based in vitro and animal models for VL. Recently, four PhD theses have been completed in the field of Leishmania, while two PhD students are presently working on drug resistance and one PhD student on the Leishmania-‐macrophage interaction. Cell-‐
based in vitro susceptibility protocols alongside animal models for L. donovani and L. infantum have been implemented for the evaluation of antileishmanial drugs. In this capacity, LMPH is collaborating closely with the Drugs for Neglected Diseases Initiative (DNDi, Geneva, Switzerland) for the evaluation and lead optimization of new antileishmanial drug development candidates. LMPH is also member of the Antwerp Drug Discovery Network (ADDN: http://www.ua.ac.be/main.aspx?c=.ADDN). LMPH possesses extended BSL-‐2 laboratory and animal facilities and is equipped with a MS200 Electron Paramagnetic Resonance spectrometer (EPR), conventional (VWR thermal cycler) and quantitative PCR equipment (StepOnePlus™ Real-‐Time PCR System, Applied Biosystems) and a flow cytometer (Cell lab quanta, Beckman Coulter). The expertise for bioanalysis using LC-‐MS2 is also present (1 FTE technical staff member) and fits within the broader objectives of the Antwerp Drug Discovery network (ADDN) and operates within the UA unit for Biomolecular Mass Spectrometry CeProMa. The expertise of the LMPH team is proven by international publications in peer-‐reviewed journals. We publish regularly in the top journals of microbiology and medicinal chemistry, like Antimicrobial Agents and Chemotherapy (IF = 4.841), Journal of Antimicrobial Chemotherapy (IF = 5.068) and Journal of Medicinal Chemistry (IF = 5.248). Prof. Maes has published over 150 scientific articles in peer-‐reviewed international journals and is one of the editors of the “Journal of Antimicrobial Chemotherapy”. Prof. Cos has published over 100 scientific articles in peer-‐reviewed international journals. He is an editorial board member of several peer-‐
reviewed journals, including “Frontiers in Fungi and their Interactions”, “Pharmaceuticals” and “Medicinal Chemistry”. Prof. Delputte has published more than 40 scientific articles in peer-‐
reviewed international journals, amongst them several in journals with an IF >5 in the field of pathogen-‐macrophage interactions, the development of monoclonal antibodies and the role of glycans and lectin receptors in these interactions. 5. Scientific methods used Please give a short description of the scientific methods available in your laboratory, with special emphasis on specialized non-‐standard methodologies possibly not available to many others in the network (max. 1000 characters, including spaces). LMPH is actively involved in a multidisciplinary consortium (www.ua.ac.be/addn) for the identification of new synthetic and natural lead compounds, with a particular focus on tropical protozoa (leishmaniasis, malaria, sleeping sickness and Chagas disease), micro-‐aerophilic intestinal pathogens (Giardia and Helicobacter), and bacterial and fungal infections (Gram-‐
positive and Gram-‐negative bacteria, yeasts, dermatophytes and fungi). Validated in vitro and in vivo laboratory models and drug screening technologies are available, enabling a valid pharmacological ‘proof of concept’. The intrinsic pharmacological activity of a drug is only a part of the in vivo activity since its pharmacokinetic properties (absorption, distribution, metabolism and excretion) play a pivotal role. Analysis of plasma and tissue using LC-‐MS/MS technology allows defining the pharmacodynamics in greater detail. In addition, bioequivalence studies allow comparison of different administration routes and drug formulations. The current set-‐up enables generation of adequate proof-‐of-‐concept. In this capacity, LMPH is also part of the antileishmanial lead-‐optimisation team of DNDi (Geneva, Switzerland). Drug resistance in visceral leishmaniasis is gradually increasing. Within the ongoing program of drug research and in collaboration with the Antwerp Institute of Tropical Medicine (ITMA), mechanisms for resistance development are elucidated in an attempt to identify drug-‐
resistance markers. For that purpose, recent clinical field isolates from treated patients and artificially induced laboratory strains are used. Bacterial biofilm formation and virulence: biofilms are defined as microbial populations (mostly bacteria and yeasts) embedded in an organic polymer matrix attached to an inert surface. In this matrix, the organisms become well protected against antibiotics and/or disinfectants. At LMPH, research focuses on the (virulence) factors that play a role in the formation of biofilms and the increase resistance to treatment using validated in vitro and in vivo models for detection and quantification of biofilms and virulence factors. 6. Publications in the field Please give full bibliography of your 5 most important scientific publications relevant to the field. 1) Monzote L. Cuesta-‐Rubio O., Campo Fernandez M., Márquez Hernandez I., Fraga J., Pérez K., Kerstens M., Maes L., Cos P.: In vitro antimicrobial assessment of Cuban propolis extracts, Memorias do Instituto Oswaldo Cruz, 2012, 107 (8), 978-‐984. 2) Deprez-‐Poulain R., Flipo M., Piveteau C., Leroux F., Dassonneville S., Florent I., Maes L., Cos P., Deprez B.: Structure-‐activity relationships and blood distribution of antiplasmodial aminopeptidase-‐1 inhibitors, Journal of Medicinal Chemistry, 2012, 55 (24), 10909-‐10917. 3) Inocêncio da Luz R., Vermeersch M., Deschacht M., Hendrickx S., Van Assche T., Cos P., Maes L.: In vitro and in vivo prophylactic and curative activity of the triterpene saponin PX-‐6518 against cutaneous Leishmania species, Journal of Antimicrobial Chemotherapy, 2011, 66 (2), 350-‐353. 4) Vermeersch M., Inocêncio da Luz R., Toté K., Timmermans J.P., Cos P., Maes L.: In vitro susceptibility of Leishmania donovani promastigote and amastigote stages to antileishmania reference drugs – practical relevance of stage-‐specific differences, Antimicrobial Agents & Chemotherapy, 2009, 53 (9), 3855-‐3859. 5) Cos P., Vlietinck A.J., Vanden Berghe D., Maes L.: Demonstration of anti-‐infective potential of natural products – how to develop a stronger in vitro ‘proof-‐of-‐concept’, Journal of Ethnopharmacology, 2006, 106, 290-‐302. 7. Existing cooperations Please list active cooperations with relevance to the field. Put special emphasis on existing cooperations with scientists who are already members of ResNet NPND. International organisations -‐ Drugs for Neglected Diseases initiative (DNDi), 1 Place Saint Gervais, 1201 Geneva, Switzerland Universities -‐ Prof. Dr. L.L. Gundersen, Department of Chemistry, University of Oslo, P.O.Box 1033, Blindern, N-‐0315 Oslo, Norway -‐ Dr. F. Epifano, Department of Pharmaceutical Sciences, Universita G. D’Annunzio di Chieti-‐
Pescara, Via dei Vestini 31, 66013 Chieti Scalo, Italy -‐ Dr. Deniz Tasdemir, School of Pharmacy, Department of Pharmaceutical and Biological Chemistry, Centre for Pharmacognosy and Phytotherapy, University of London, Brunswick Square 29-‐39, London WC1N 1AX, UK -‐ Dr. Jean-‐Robert Ioset, Laboratoire de Pharmacognosie et Phytochimie, Université de Genève, Quai Ernest-‐Ansermet 30, 1211 Genève -‐ Dr. Lianet Monzote Fidalgo, Parasitology Department, Tropical Medicine Institute “Pedro Kouri”, Havana, Cuba -‐ Dr. J. Sarlauskas, Institute of Biochemistry, Mokslininku street 12, Vilnius, Lithuania -‐ Dr. E. Davioud-‐Charvet, Biochemie-‐Zentrum Heidelberg, Im Neuenheimer Feld 504, 69120 Heidelberg, Germany -‐ Dr. B. Déprez, Biostructures et Découverte de Médicament, Unité mixte Inserm-‐Lille2-‐Institut Pasteur de Lille, 3 rue du Professeur Laguesse, 59006 Lille, France -‐ Prof. Dr. T. Kurz, Universität Hamburg, Institut der Pharmazie, Bundesstrasse 45, 20146 Hamburg, Germany -‐ Prof. Dr. A. Gasco, Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via Pietro Giuria 9, 10125 Torino, Italy -‐ Dr. M. Sauvain, Research Director (UMR-‐152), Mission IRD, Casilla 18, 1209 Lima 18, Peru and Prof. G. Arevalo, Universidad Peruana Cayetano Heredia, Lima, Peru -‐ Dr. S. Botti, Parco Tecnologico Padano – CERSA, Integrative Biology Group, Via A. Einstein, 26900 Lodi, Italy -‐ Dr. S. M. Al-‐Massarani, King Saud University, College of Pharmacy, Dept. of Pharmacognosy, P.O. Box 2457, Riyadh 11451, Saudi Arabia 8. Expectations Please give a short outline on (a) what you expect from a membership and active contribution to ResNet NPND and (b) what ResNet NPND can expect from you (max. 500 characters, including spaces). Our research group LMPH is seeking for new molecules with clinically relevant biological activities for further evaluation in joint projects. We are also interested to unravel the mechanism-‐of-‐action/pharmacodynamics of these bioactive molecules and contribute to generation of a strong proof-‐of-‐concept. 9. Commitment Please give a short outline on what ResNet NPND can expect from you in case your application is accepted; please also make an estimate on the importance of work in this field for your total scientific work (e.g. in % of your total workload or output) (max. 500 characters, including spaces). In the framework of this network we are willing to participate in joint project proposals to get research funding. 10. Declaration of scientific independence and signature I hereby confirm this application with my legal signature. At the same time I declare, that I am legally authorized to conduct own research projects, coordinate joint research, publish data and work independently in a scientific environment. I also declare that I commit myself to the aims and goals of ResNet NPND. I understand that I have the right to terminate my membership at any time, which in this case I must do in written form, to a member of the executive board. Antwerp, 15-‐01-‐2014 L. Maes P. Cos P. Delputte ____________________________________________________________________ (Place) (Date) (Signature) Please fill in, print and sign this form. It can be sent back as hardcopy or, preferably, as a scanned pdf document to thomschm@uni-‐muenster.de Application for membership in ResNet NPND
(This document is accompanied by a document with some formal rules and explanations about the
network as well as a copy of the ResNet NPND Memorandum of Commitment signed by the founding
members in 2011. Please read this document carefully and then fill in the following form).
Please type requested informations
Kang
Name
Jong Seong
First name
Professor
Academic title(s)
Institution: Chungnam National University
Daehakro 99, Yuseong-Gu, Daejeon, 305-764 Korea
Department: College of Pharmacy
Function: Professor
3. Statement of motivation
I am interested in the neglected disease and development of new drug for the treatment of
Chagas disease and leishmaniasis. Dr. Schmidt recommended me to join ResNet NPND in 2013.
4. Expertise and experience in the field
I have experience in the field of herbal drug development, especially analysis of new
compound, standardization of herbal drugs, fingerprint analysis of herbs, statistical treatment
of the data.
5. Scientific methods used
Spectroscopic and chromatographic methods to isolate and to analyze the specific compounds
in the natural products. Statistical tools for the evaluation of obtained data.
6. Publications in the field
Please give full bibliography of your 5 most important scientific publications relevant to the field.
1.
2.
3.
4.
5.
Quantitative Determination of Marker Compounds and Pattern Recognition Analysis for Quality
Control of Alismatis Rhizoma by HPLC. Bull. Kor. Chem. Soc. 2013, 34(7), 2081-5.
Chemical-based Species Classification of Rhubarb Using Simultaneous Determination of Five
Bioactive Substances by HPLC and LDA Analysis. Phytochemical Analysis 2012, 23, 359-364
Multiple Component Quantitative Analysis for the Pattern Recognition and Quality Evaluation
of Kalopanacis Cortex Using HPLC. Arch. Pharm. Res. 34(12), 2065-2071 (2011).
Comparative pharmacokinetics of three marker compounds in mBHT and single-herb extract
after oral administration to rats. J. Pharm. Biomed. Anal. 56 (2011) 1121– 1126.
Determining the pharmacokinetics of psilocin in rat plasma using ultra-performance liquid
chromatography coupled with a photodiode array detector after orally administering an extract
of Gymnopilus spectabilis. J. Chromatogr. B 879 (2011) 2669 - 2672.
7. Existing cooperations
NRF-DAAD Partnership program (Korea and Germany) with Professor Schmidt, in Muenster, Germany is
running since Sep. 2013. The title of program is “New natural compounds from Korean and German
plants with activity against Trypanosoma species responsible for neglected tropical diseases”
8. Expectations
Please give a short outline on (a) what you expect from a membership and active contribution to ResNet
NPND and (b) what ResNet NPND can expect from you (max. 500 characters, including spaces).
I want to share the valuable information about neglected disease and related fields through the
network, and exchange the samples and results of activity tests with other researchers in other
countries. I hope that my knowledge about neglected disease acquired by joining ResNet NPND could be
helpful to relieve the patients from the neglected disease in East Asia.
9. Commitment
The present ResNet NPND members are mostly working in the field of pharmacognosy or biology.
However, the experts from various fields - target discovery, medicinal chemistry, pharmaceutical
sciences etc. – have to participate in the network to realize the development of new drug to treat the
neglected disease. I can develop analytical methods to control the quality of raw materials and products
in the IND or further stage of drug development. Furthermore I have a good collaboration with the
researchers in Asian countries. If my application is accepted, I will put my effort over 30% of my scientific
work.
10. Declaration of scientific independence and signature
I hereby confirm this application with my legal signature.
joint research, publish data and work independently in a scientific environment. I also declare that I
commit myself to the aims and goals of ResNet NPND.
Daejeon
Nov. 26. 2013
____________________________________________________________________
(Place)
(Date)
(Signature)
Application for membership in ResNet NPND
Name Khalid
First name Sami
Academic title(s) Professor
Institution: Faculty of Pharmacy, University of Science & Technology
Affiliated Professor, Faculty of Pharmacy, University of Khartoum
Department: Pharmacognosy & Phytochemistry
Function: Teaching, Research and administrative duties as dean of the Faculty of Pharmacy
Please type a statement explaining your motivation to join ResNet NPND (max. 1000 characters,
including spaces).
My involvement in the drug discovery of natural products against neglected diseases dating back to
1985 and our first paper addressing this topic appeared in 1986. Since then I managed to persuade a
number of prominent scientists in both developing and developed countries to come on board and
collaborate on tackling this neglected devastating diseases and as a result a number of contributions
(e.g. papers, presentations, book chapter, reviews) were made. Due to the pressing need to promote
activities on natural products chemistry at a regional level we took the initiative to formulate Natural
Products Research Network for Eastern and Central Africa (NAPRECA) in 1984. Since its inception
th
NAPRECA organized 15 international symposia in Africa and I had the privilege to organize the 15
symposium in Khartoum (Sudan) in December 2013.
Please give a short description of your scientific background, expertise and experience in the field of
natural products, neglected diseases or, optimally, both (max. 1000 characters, including spaces).
My research has generally been directed towards the isolation of plant secondary metabolites with
special emphasis on traditionally used antiparasitic medicinal plants and their bioactive agents. A wide
range of natural products have been isolated and their structures fully elucidated using modern
spectroscopic techniques. Particular expertise has been developed on the interpretation of nuclear
1
13
magnetic resonance spectroscopy ( H & C NMR), including high field (400 and 600 MHz) one- and twodimensional multi-pulse NMR spectroscopy and hyphenated techniques (e.g. GC/MS/MS & LC/MS/MS).
Compounds isolated and structurally identified include alkaloids; flavonoids, chromones, coumarins,
lignans, naphthopyrans, sesquiterpene, diterpenes, triterpenes, saponins and limonoids. A sizable
portion of the research, post 1985, was directed to the investigation of the antiprotozoal activity of
medicinal plants with special emphasis on NDs.
Please give a short description of the scientific methods available in your laboratory, with special
emphasis on specialized non-standard methodologies possibly not available to many others in the
network (max. 1000 characters, including spaces). In addition to the basic chromatographic setting for
detection and isolation, we have established a small facility for the screening antileishmanial activity
against both the promastigote and amastigotes of L. tropica, L. major and L. donovani. We are currently
measuring the intracellular activity of the extracts/compounds by monitoring the immunomodulatory
activity inside the macrpophages. The antimalarial and antitrypanosmal activities are tested in our
labrotory by microtiter-based screening utilizing enoyl-ACP reductase (PfENR) and trypanothione
reductase (TryR), respectively.
1. Bedri, S.; Khalil, EA.; Khalid, SA.; Alzohairy, MA.; Mohielden, A.; Aldebasi, YH.; Seke etet, PF.; Farahna, M.
Azadirachta indica ethanolic extract protects neurons from apoptosis and mitigates brain swelling in experimental
cerebral malaria. Malaria Journal, 2013, 12:298, doi:10.1186/1475-2875-12-298.
2. Khalid, S.A. Natural products-based drug discovery against neglected diseases with special reference to African
natural resources. In “Drug Discovery in Africa”. (Eds Chibale, K., Masimirembwa, C. and Davies-Coleman, M.).
Springer-verlag, 211-237, 2012.
3. Schmidt, T. J., Khalid, S. A., Romanha, A. J., Alves, T.M.A. Biavatti, M. W. Brun, R.,. et al. The potential of
secondary metabolites from plants as drugs/leads against protozoan neglected diseases - Part I, Current Medicinal
Chemistry, 19, 2128-2175, 2012. Part II, Current Medicinal Chemistry, 19, 2176-2228, 2012.
4. Khalid,S.A., Friedrichsen,G.M., Kharazmi, A., Theander, T. and Christensen, S.B and Olsen, CE. Limonoids from
Khaya senegalensis, Characterization of 2”, 6-dihydroxy-fissinolide as a new limonoid. Phytochemistry , 49, 17691772, 1998.
5. Khalid, S.A., Duddeck, H. and GonzalezSierra, M. Isolation and Characterization of the antimalarial
agent of the Neem tree , Azadirachta indica. J. Nat. Prod., 52, 922-927, 1989.
Please list active cooperations with relevance to the field. Put special emphasis on existing cooperations
with scientists who are already members of ResNet NPND.
We had established a strong collaboration with the Swiss Tropical Institute, Basel, Switzerland since the
1993 and lately with WHO/TDR, Geneva, Switzerland. Our main currently active collaboration is with
Professor Schmidt, T. J of the Institut für Pharmazeutische Biologie und Phytochemie, Münster,
Germany.
8. Expectations
I would anticipate a development of network-wide training activities (e.g. workshops, summer schools)
that exploit the interdisciplinary aspects and provision of structured training courses within the
framework of a joint training program with other networks in Africa such as NAPRECA. This should
include exchange of knowledge through undertaking visits and secondments. A strong networking
component should be required in each proposal.
9. Commitment
Please give a short outline on what ResNet NPND can expect from you in case your application is
accepted; please also make an estimate on the importance of work in this field for your total scientific
work (e.g. in % of your total workload or output) (max. 500 characters, including spaces).
I would spare no efforts to establish strong networking ties with NAPRECA in my current capacity as an
Executive Secretary of the Coordinating Office. I presume that the establishment of such a link would
take substantial time and efforts for its realization. It is quite difficult, however, to estimate the total
workload at this stage.
Khartoum, 22 January 26, 2014______________________________________________________
(Place)
(Date)
(Signature)
Please fill in, print and sign this form. It can be sent back as hardcopy or, preferably, as a scanned
pdf document to thomschm@uni-muenster.de
Kim
Name
Young Ho
First name
Professor
Academic title(s)
Institution: Chungnam National University
Daehakro 99, Yuseong-Gu, Daejeon, 305-764 Korea
Department: College of Pharmacy
Function: Professor
Please type a statement explaining your motivation to join ResNet NPND (max. 1000 characters,
including spaces).
In deep concern about neglected diseases especially in Asia and Africa, Dr. Schmidt
recommended me to join ResNet NPND in 2013.
Please give a short description of your scientific background, expertise and experience in the field of
natural products, neglected diseases or, optimally, both (max. 1000 characters, including spaces).
Much experience in the field of screening, bioassay, isolation and structure elucidation from
natural products.
Please give a short description of the scientific methods available in your laboratory, with special
emphasis on specialized non-standard methodologies possibly not available to many others in the
network (max. 1000 characters, including spaces).
Isolation of active compounds from natural products
Structure elucidation of organic compounds from natural origin
1.
2.
3.
4.
5.
Anti-inflammatory Asterosaponins from the Starfish Astropecten monacanthus. J. Nat. Prod.
2013, 76, 1764−1770
NF-κB Inhibitory Activity of Sucrose Fatty Acid Esters and Related Constituents from Astragalus
membranaceus. J. Agric. Food Chem. 2013, 61, 7081−7088.
Scopoletin and Scopolin Isolated from Artemisia iwayomogi Suppress Differentiation of
Osteoclastic Macrophage RAW 264.7 Cells by Scavenging Reactive Oxygen Species. J. Nat.
Prod. 2013, 76, 615−620.
Anti-inflammatory and PPAR Transactivational Effects of Components from the Stem Bark of
Ginkgo biloba. J. Agric. Food Chem. 2012, 60, 2815−2824
. Anti-inflammatory Triterpenoid Saponins from the Stem Bark of Kalopanax pictus. J. Nat.
Prod. 2011, 74, 1908–1915
NRF-DAAD Partnership program (Korea and Germany) with Professor Schmidt, in Muenster,
Germany is running since Sep. 2013. The title of program is “New natural compounds from
Korean and German plants with activity against Trypanosoma species responsible for neglected
tropical diseases”
8. Expectations
I expect that I have much valuable information about neglected disease from this network, and share
research interest about neglected disease and cooperate together in network system. I hope my effort
will be a small contribution for treatment of neglected disease
Neglected diseases are serious problem in Asia. With my joining in ResNet NPND, new information and
research in Aisa will be shared and can be explored big interest about neglected disease in Asia region.
9. Commitment
Please give a short outline on what ResNet NPND can expect from you in case your application is
accepted; please also make an estimate on the importance of work in this field for your total scientific
work (e.g. in % of your total workload or output) (max. 500 characters, including spaces).
ResNet NPND can enlarge interest about neglected disease including Asia, and possible strong network
in Aisa region. We can make good results with high potency in this field and possible to have good
collaborations together in network system.
If my application is accepted, estimation of my total scientific work will be over 50%.
Daejeon
Nov. 26. 2013
____________________________________________________________________
(Place)
(Date)
(Signature)
(This questionnaire is accompanied by a document with some formal rules and explanations about the
Nonato
Maria Cristina
Name
First name
PhD
Academic title(s)
Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto
Department: Departamento de Física e Quimica
Function: Associate Professor
I am the head of the Protein Crystallography Laboratory of Ribeirão Preto (LCP-RP), a city located in the
country side of São Paulo state. At LCP, we are deeply interested in contributing to the development of
new therapies against neglected diseases. We believe that our expertise in the field and the projects we
work with can greatly contribute to characterize the mechanism of action of molecules already identified
by ResNet NPND as active compounds.
The Protein Crystallography Lab works in the structural and functional characterization of proteins with
pharmaceutical and biotechnological interest. In particular, the lab is interested on target validation and
development of new therapies against neglected diseases such as Chagas´disease, Leishmaniasis and
Schistosomosis.
Through the use of a multidisciplinary approach combining in vitro, in silico and in vivo techniques, as
recombinant DNA technology, X-ray crystallography and Biophysics, biochemistry and cell biology tools,
the projects under development seek to contribute to the mapping of the mechanism of action of
proteins, as well as the validation of new pharmaceutical targets and the identification of potent and
selective ligands for the development of a formulation to be use in our and pre-clinical assays.
At LCP we use a combination of in vitro and in silico techniques for characterization of molecular targets
against neglected diseases and the development of new drug prototypes against Chagas´disease,
Leishmaniasis and Schistosomiasis. In particular we work with:
Xray Crystallography
Biophysical Methods: CD (Circular Dichroism), ESR (Electron Paramagnetic Ressonance) , DLS( Dynamic
Ligh Scaterring)
Molecular Dynamics
Docking
Screening of ligands by Flurescence Thermo assays and Elisa Asssays
Molecular Biology ( site-direct mutagenesis, knock outs)
1.
CHELESKI, J.; ROCHA, J.R.; PINHEIRO, M.P.; WIGGERS, H.J.; SILVA, A.B.F.; NONATO, M.C.; MONTANARI,
C.A. Novel insights for dihydroorotate dehydrogenase class 1A inhibitors discovery. European Journal of
Medicinal Chemistry, v.45, p.5899-5909, 2010.
2. CHELESKI, J.; WIGGERS, H.J.; CITADINI, A.P.; COSTA FILHO, A.J.; NONATO, M.C.; MONTANARI, C.A. Kinetic
mechanism and catalysis of Trypanosoma cruzi dihydroorotate dehydrogenase enzyme evaluated by
isothermal titration calorimetry. Analytical Biochemistry, v.399, p.13 - 22, 2010.
23. FELICIANO, Patrícia Rosa; GUPTA, Shreedhara; DYSZY, Fabio; DIAS BARUFFI, Marcelo; COSTA FILHO,
Antonio José; MICHELS, Paul A.M.; NONATO, Maria Cristina. Fumarate hydratase from Leishmania
major: subcellular localization, structural and kinetic properties. International Journal of Biological
Macromolecules, v. 51, p. 25-31, 2012.
24. CORDEIRO, Artur Torres; FELICIANO, Patrícia Rosa; PINHEIRO, Matheus Pinto; NONATO, Maria Cristina.
Crystal structure of dyhidroorotate dehydrogenase from Leishamania major. Biochimie, v. 94, p. 173948, 2012.
25. PINHEIRO, Matheus Pinto; EMERY, Flávio S.; NONATO, Maria Cristina. Target sites for the design of antitrypanosomatid drugs based on the structure of dyhidroorotate dehydrogenase. Current Pharmaceutical
Design. v. 19, p. 2615-2627, 2013.
We have just started collaborating with Prof. Fernando Batista da Costa, by screening his extracts of
Brazilian Asteraceae against our validated targets.
8. Expectations
We expect to increase the chemical diversity of the compounds tested against our enzymes.
We offer to the members of the ResNet NPND the possibility of testing a high number of compounds
against our parasite targets and human homologue proteins and characterize thire mechanism of
inhibition by kinetic and structural approaches. Those results will allow us to design new molecules with
improved both binding efficacy and selectivity as an important step towards drug development.
9. Commitment
Drug development against neglected disease is the main area of research ofin our laboratory. There are
many projects under development and we will certainly get more experience in the field in the following
months by learning how to perform our first pre-clinical assays. ResNet NPND can expect that we wil
continue to work on the field and devote 100% of our scientific work on the application and developing
new methodologies to characterize and validate new targets as well as search for ligands as prototypes
for drug development. We are deeply interested in collaborating with people from the field covering the
most broad aspects and methodologies of drug discovery.
Ribeirao Preto, December 5th, 2013
____________________________________________________________________
(Place)
(Date)
(Signature)
I
(This questionnaire is accompanied by a document with some formal rules and explanations about the
network as well as a copy of the ResNet NPND Memorandum of Commitment Signed by the founding
members in 2011. Please read this document carefully and then fill in the following form)'
1..
Personalinformation
Name
2.
Affiliation
NWODO
-
First name NGOZI
JUSTINA
Academic title(s)DR
lnstitution, Department, Function
lnstitution: University of Nigeria, Nsukka
Department: Pharmaceutical and Medicinal Chemistry
Function: Lecturing
3.
Statement of motivation
Please type
o stotement exptoining your motivotion
to
ioin ResNef NPND (mox. 7000 charocters,
inctuding spoces).
My motivation is based on the quality of the scientist in the network. I believe that someday
noble outcome willemerge from this group and lwill be part and parcelof the success. My
scope of collaboration will also increase from this network.
4.
a
Expertise and experience in the field
o short description of your scientific bockground, expertise ond experience in the field of
products,
negtected diseases or, optimally, both (mox. 1000 choracters, including spoces).
notural
please give
My area of specialization is on Natural product chemistry, with'bias on trypanocidal plants,
where did my Ph.D research. Majority of my research works are on trypanocidal properties of
pla nts.
Application for membership in ResNet NPND (This questionnaire is accompanied by a document with some formal rules and explanations about the network as well as a copy of the ResNet NPND Memorandum of Commitment signed by the founding members in 2011. Please read this document carefully and then fill in the following form). Please type requested informations 1. Personal information Ogungbe Name Ifedayo Victor First name Assistant Professor Academic title(s) 2. Affiliation – Institution, Department, Function Institution: Jackson State University, Jackson, MS, USA Department: Chemistry and Biochemistry Function: Teaching, Research and Service 3. Statement of motivation Please type a statement explaining your motivation to join ResNet NPND (max. 1000 characters, including spaces). I have strong research interest in natural products‐based medicinal chemistry, chemical biology and cheminfomatics. I have and will continue to contribute to drug discovery programs targeting tropical diseases. I started my independent research career last year, and I think ResNet NPND is a very good platform to connect, interact and collaborate with researchers that are interested in tropical diseases especially the neglected ones. 4. Expertise and experience in the field Please give a short description of your scientific background, expertise and experience in the field of natural products, neglected diseases or, optimally, both (max. 1000 characters, including spaces). I have academic degrees in Chemistry, Biochemistry, and Biotechnology Engineering. My research endeavors includes isolation and characterization of natural products, in vitro and in silico drug target‐ based screening, modeling of target‐ligand interactions, and target characterization (biochemical and structural biology). I am interested in all tropical disease but my focus diseases are Trypanosomiasis, Leishmaniasis and Malaria. 5. Scientific methods used Please give a short description of the scientific methods available in your laboratory, with special emphasis on specialized non‐standard methodologies possibly not available to many others in the network (max. 1000 characters, including spaces). 1. We have tools and equipments for a. natural products isolation and characterization b. basic molecular biology work and target‐based screening* c. small scale organic synthesis 2. We also have licenses for homology modeling, molecular docking and QSAR softwares *Since it’s a young lab we are slowly build up. 6. Publications in the field Please give full bibliography of your 5 most important scientific publications relevant to the field.
1. Ogungbe IV, Erwin WR, Setzer WN. Antileishmanial phytochemical phenolics: Molecular docking to potential protein targets. J Mol Graph Model. 2014 Mar;48:105‐
17. 2. Ogungbe IV, Ng JD, Setzer WN. Interactions of antiparasitic alkaloids with Leishmania protein targets: a molecular docking analysis. Future Med Chem. 2013 Oct;5(15):1777‐
99. doi: 10.4155/fmc.13.114. 3. Ogungbe IV, Setzer WN. In‐silico Leishmania target selectivity of antiparasitic terpenoids. Molecules. 2013 Jul 3;18(7):7761‐847. 4. Setzer WN, Ogungbe IV. In‐silico investigation of antitrypanosomal phytochemicals from Nigerian medicinal plants. PLoS Negl Trop Dis. 2012; 6(7):e1727. 5. Ogungbe IV, Hill GM, Crouch RA, Vogler B, Nagarkoti M, Haber WA, Setzer WN. Prenylated isoflavonoids from Rhynchosia edulis. Nat Prod Commun. 2011 Nov;6(11):1637‐44. 7. Existing cooperations Please list active cooperations with relevance to the field. Put special emphasis on existing cooperations with scientists who are already members of ResNet NPND. I have active collaborations and mutual research projects with Dr. William Setzer (University of Alabama in Huntsville, USA and My PhD Advisor). I am also developing some collaboration in the field. 8. Expectations Please give a short outline on (a) what you expect from a membership and active contribution to ResNet NPND and (b) what ResNet NPND can expect from you (max. 500 characters, including spaces). a. I expect to develop active collaborations, and nurture synergistic and mutually beneficial research projects with interested members. b. I will provide time and resources as much as possible to advance the scientific, professional and positive societal objectives of the network. 9. Commitment Please give a short outline on what ResNet NPND can expect from you in case your application is accepted; please also make an estimate on the importance of work in this field for your total scientific work (e.g. in % of your total workload or output) (max. 500 characters, including spaces). 50% of my young program is dedicated to research in this field. Declaration of scientific independence and signature I hereby confirm this application with my legal signature.
At the same time I declare, that I am legally authorized to conduct own research projects, coordinate joint research, publish data and work independently in a scientific environment. I also declare that I commit myself to the aims and goals of ResNet NPND. I understand that I have the right to terminate my membership at any time, which in this case I must do in written form, to a member of the executive board. Jackson 02/18/2014 ____________________________________________________________________ (Place) (Date) (Signature) Please fill in, print and sign this form. It can be sent back as hardcopy or, preferably, as a scanned pdf document to thomschm@uni‐muenster.de

Read Members` reports Sept 2011

Transcription

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