alpha-arbutin - Lotioncrafter

ALPHA-ARBUTIN
Superior skin lightening enhancer
for a perfect even skin tone
The quest for a
lighter skin tone
Mechanism
In many regions of the world, the concept of beauty is inseparably
linked to a light skin tone. The biggest concern for consumers is finding
the right product. DSM has addressed this demand with ALPHA-ARBUTIN,
which has proven itself the perfect choice for those seeking a lighter,
even skin tone. Thanks to its high efficacy, ALPHA-ARBUTIN has gained
wide acceptance and is rated highly by people from all walks of life.
ALPHA-ARBUTIN has been specially developed to ensure a lighter skin
tone. Unique, high-performing, enzyme-related biotechnology
guarantees high purity, addressing increased consumer awareness
about safety and efficacy.
Cosmetic products with ALPHA-ARBUTIN typically activate skin lightness
by inhibiting tyrosinase, one of the major enzymes involved in the
formation of skin tan and age spots. The first visible results can be
expected after four weeks, in contrast with other Arbutins like
Beta-Arbutin, which take longer to achieve results. In vivo studies also
demonstrate that ALPHA-ARBUTIN reduces the degree of skin tanning
after UV exposure and helps to minimize the appearance of liver spots.
Key facts
Unique product features
• Scientifically proven effects at low concentrations
- More effective at 1.0% than Beta-Arbutin in vivo
- Nine times more effective than Beta-Arbutin in vitro
- Outstanding tyrosinase inhibition activity in vitro
• Highly pure biosynthetic active ingredient
• High performing enzyme related biotechnology
Benefits
• Ensures an even, lighter skin tone
• Reduces the degree of skin tanning after UV exposure
• Helps to minimize the appearance of liver spots
Structurally, ALPHA-ARBUTIN (chemical name: 4-hydroxyphenyl-α-Dglucopyranoside) is an α-glucoside compared to the β-form of the
related beta-arbutin.
ALPHA-ARBUTIN
Beta-Arbutin
The α-glucoside bond offers higher efficacy than the β-form. In vitro
tests show that ALPHA-ARBUTIN exhibits impressive tyrosinase
inhibition and is nine times more effective than Beta-Arbutin. Very low
IC50 values (the concentration that produces a 50% inhibition of
human tyrosinase) indicates the power of ALPHA-ARBUTIN.
ALPHA-ARBUTIN: IC50 = 1.0 mMol Beta-Arbutin: IC50 = 9.0 mMol
The outstanding efficacy of ALPHA-ARBUTIN is due to its perfect affinity
to the active site of tyrosinase. DFT (density functional theory)-optimized
structures and ESP (electrostatic potential) calculations on ALPHAARBUTIN, Beta-Arbutin, and the substrate of tyrosinase, tyrosine,
reveals that the ESP for ALPHA-ARBUTIN is similar to that of tyrosine.
The ESP potential for Beta-Arbutin indicates potential difficulties when binding
to tyrosinase, meaning the inhibitory activity of Beta-Arbutin is low1.
Tyrosinase
Tyrosinase
Dopa
Dopaquinone
ALPHA-ARBUTIN
Melanin
Tyrosine
Cosmetic application
INCI name (active)
Alpha-Arbutin
Beta-Arbutin
0.9
0.7
0.6
0.5
0.4
Fig. 1: DFT (density functional theory)-optimized structures and calculated ESP’s.
0.3
The yellow dots represent the negative regions and the blue dots represent the
0.2 regions of the electrostatic potential.
positive
0.1
1 Sugimoto
Kazuhisa et al., Ezaki Glico Co., Ltd., Biochem. Res. Lab., JPN
0
ALPHA-ARBUTIN
50
45
Markedly improved
Kojic acid
Improved
Beta-Arbutin
Slightly improved
Hydroquinone
Ineffective
5
Aggravated
4.5
40
4
35
3.5
30
25
20
15
Tanning ΔL
• Up to 2% for face and neck preparations
Tyrosine
0.8
Lightening (%)
Suggested concentration
ALPHA-arbutin
1.0
Liver spot reduction (%)
• Intensive skin lightening products
• Even skin tone care
• Age spot treatment
• BB/CC creams
3
2.5
2
1.5
10
1
5
0.5
one
Dopaquino
Dopa
ALPHA-ARBUTIN
Efficacy
Melani
1.0
0.9
Tyrosinase
Tyrosine
Tyrosinase
One-month skin lightening study
0.8
0.7
Dopaquinone
Liver0.6spot study
Dopa
Four emulsions containing ALPHA-ARBUTIN, Kojic acid, BetaArbutin and Hydroquinone at 1% use level respectively were
applied twice a day for one month on the forearm of 80 women
ALPHA-ARBUTIN
of Chinese descent. The parameter L which represents the
lightness of skin was determined by means of chromameter.
1.0
0.9
Lightening (%)
In vivo
0.5
A three-month study was performed on 26 women (aged between
0.4
40 and 65) with liver spots. Creams including test substances were
0.3
applied
twice daily on different test areas. After three consecutive
Melanin
0.2
months of application, the liver spot reduction efficacy was evaluated
0.1 eye using the following five-grade scale: markedly
with the
0
improved,
slightly improved, ineffective and aggravated . 53.7% of
ALPHA-ARBUTIN
Kojic acid
Beta-Arbutin
Hydroquinone
the panellists
reported a markedly
improved
or improved
condition
with ALPHA-ARBUTIN against only 30.6% for Beta-Arbutin2.
50
0.7
Dopaquinone
0.5
0.4
0.3
0.2
0.1
Melanin
0
ALPHA-ARBUTIN
Kojic acid
Beta-Arbutin
Hydroquinone
Markedly improved
Improved
Slightly improved
Ineffective
Aggravated
ALPHA-ARBUTIN ensures a lighter skin tone when compared with
40
Beta-Arbutin, Kojic acid and Hydroquinone at 1% use level.
Ineffective
35
3.5
30
25
20
5
10
1
5
0.5
0
5
2% ALPHA-ARBUTIN
0
2% Beta-Arbutin
0% ALPHA-ARBUTIN cream
Fig. 3: Satisfaction quotients relating to the evaluation
of the liver spot reduction
4.5
1% ALPHA-ARBUTIN cream
2% ALPHA-ARBUTIN cream
Results:
4
Tanning ΔL
2
1.5
1
0.5
0
1 week
2 weeks
0% ALPHA-ARBUTIN cream
1% ALPHA-ARBUTIN cream
2% ALPHA-ARBUTIN cream
4
Tanning ΔL
3.5
3
2.5
2
.
1.5
1
0.5
0
1 week
2 weeks
Fig. 4: ΔL values for ALPHA-ARBUTIN creams one and two weeks after UV exposue
Results:
ALPHA-ARBUTIN reduces the degree of skin tanning after UV exposure.
2
1.5
3
2 H. Ziegler et al., “The More Effective, Faster and Safer Approach to Skin Lightening and Liver Spot
Minimizing,”
2.5 PERSONAL CARE (Jan 2003): 15–18
4.5
3
2.5
15
3.5
ALPHA-ARBUTIN
helps to minimize liver spots.
25
4.5
4
30
A double
blind study was performed on 23 healthy volunteers.
20
The inside
of the upper arm of each volunteer was irradiated with
15
ultraviolet
rays
(1.4 MED) using a solar simulator, and immediately
10
thereafter test samples with ALPHA-ARBUTIN (1% and 2%) were
5
applied twice a day for two consecutive weeks. Skin color (ΔL value)
0
was evaluated by
of chromameter one 2%
and
two weeks after
2% means
ALPHA-ARBUTIN
Beta-Arbutin
the end of UV exposure.
5
Aggravated
35
Skin tanning reduction after UV exposure
avated
Slightly improved
40
Fig. 2: Interaction curve for parameter “L”: treated zone vs control, difference
M1 = after one month /M0 = start (%)
Results:
45
Improved
Tanning ΔL
0.6
50
Markedly improved
45
Liver spot reduction (%)
Lightening (%)
0.8
Liver spot reduction (%)
se
Tyrosine
Europe
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P.O. Box 2676, 4002 Basel
Switzerland
Phone: +41 61 815 7777
Fax:
+41 61 815 7860
Email:info.pc-emea@dsm.com
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2 Havelock Road #04-01
Singapore 059763
Phone: +65 6632 6617
Fax:
+65 6632 6600
Email: info.pc-apac@dsm.com
North America
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45 Waterview Boulevard, Parsippany, NJ 07054
United States of America
Phone: +1 800 526 0189
Fax:
+1 973 257 8580
Email: info.pc-na@dsm.com
Latin America
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Av. Engº Billings, 1729 Prédio 31
Jaguaré – São Paulo – SP – Brasil 05321-010
Phone: + 55 11 3760 6409
Fax:
+ 55 11 3760 6492
Email: info.pc-latam@dsm.com
© 2013 DSM Nutritional Products AG, 4002 Basel, Switzerland. www.dsm.com/personal-care
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