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Alpha Arbutin Brochure
Alpha Arbutin Brochure
Alpha Arbutin Brochure
Mechanism
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
Beta-Arbutin
0.9
0.7
0.6
0.5
0.4
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
Tyrosine
0.8
Lightening (%)
Suggested concentration
ALPHA-arbutin
1.0
3
2.5
2
1.5
10
0.5
one
Dopaquino
Dopa
ALPHA-ARBUTIN
Efficacy
Melani
1.0
0.9
Tyrosinase
Tyrosine
Tyrosinase
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
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
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:
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
avated
Slightly improved
40
Results:
45
Improved
Tanning L
0.6
50
Markedly improved
45
Lightening (%)
0.8
se
Tyrosine
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