ALPHA-ARBUTIN

Superior skin lightening enhancer

for a perfect even skin tone

Exclusive N.A. Distributor

CENTERCHEM, INC. NORWALK, CT
Ph: 203-822-9800 Fax: 203-822-9820
www.centerchem.com

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--Dglucopyranoside) is an -glucoside compared to the -form of the
related beta-arbutin.
ALPHA-ARBUTIN

Beta-Arbutin

The -glucoside bond offers higher efficacy than the -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 ESPs.

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

Aggravated

4.5

40

35

3.5

30
25
20
15

Tanning L

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

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

10

0.5

0
5

2% ALPHA-ARBUTIN

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 L

2
1.5
1
0.5
0

1 week

2 weeks

0% ALPHA-ARBUTIN cream
1% ALPHA-ARBUTIN cream
2% ALPHA-ARBUTIN cream

Tanning L

3.5
3
2.5
2

1.5
1
0.5
0

1 week

2 weeks

Fig. 4: L 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): 1518

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 (L value)
0
was evaluated by
of chromameter one 2%
and
two weeks after
2% means
ALPHA-ARBUTIN
Beta-Arbutin
the end of UV exposure.

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 L

0.6

50

Markedly improved

45

Liver spot reduction (%)

Lightening (%)

0.8

Liver spot reduction (%)

se

Tyrosine

Europe

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Switzerland
Phone: +41 61 815 7777
Fax:
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Email: info.pc-emea@dsm.com

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Phone: +65 6632 6617
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Email: info.pc-apac@dsm.com

North America

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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. Eng Billings, 1729 Prdio 31
Jaguar So 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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and all liability in connection with your product or its use.
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