Arbutin
Botanical Source: Arctostaphylos uva-ursi
Part Used: Dried leaf
Specification: Arbutin 20%,99.5% By HPLC
CAS No.: 497-76-7
Molecular Formula: C12H16O7
Molecular Weight: 272.25
Melting Point: 199~201(±0.5)ºC
optical rotation: [α]D20=-64.00±1.00
Molecular Stucture:
Brief Introduction
Arbutin is a derivative of hydroquinone naturally found in some evergreen plants. As a derivative of hydroquinone, arbutin is banned in dietary aids because of toxicity. However, it is considered a non-phenol alternative to hydroquinone for dermatologic and cosmetic use. In topical applications, arbutin reduces pigmentation in the skin and has been used as a skin-lightening agent since the 1960s. Currently arbutin is combined with other active ingredients in skin-care regimens to treat dark patches from sun exposure, freckles, liver spots and age spots.
Arbutin is a glycoside; a glycosylated hydroquinone extracted from the bearberry plant in the genus Arctostaphylos. It inhibits tyrosinase and thus prevents the formation of melanin. Arbutin is therefore used as a skin-lightening agent. Arbutin is found in wheat, and is concentrated in pear skins. It is also found in Bergenia crassifolia. Arbutin was also produced by an in vitro culture of Schisandra chinensis.
Significance
Arbutin is extracted from the leaves of various types of plants, most notably the bearberry plant (Arctostaphylas uva-ursi), cranberries and blueberries, as well as in wheat and pear skins. Arbutin is converted by the body to hydroquinone, which is a type of phenol with disinfecting and diuretic properties. Arbutin was found in teas, tinctures and capsules as bearberry extracts or uva ursi extracts for weight control and menstruation aids before an FDA ban in 1990. Currently, arbutin is available in topical formulations for skin lightening because of little to no systemic absorption.
Function:
Arbutin is a glucosulated hydroquinone, extracted from the bearberry plant. Hydroquinone has been commercially available since the 1960s as an agent in skin lightening products.1 Arbutin is naturally found in wheat, pear skins, and the leaves of blueberries and cranberries, and it is metabolized by the body to produce hydroquinone with most of the product excreted in urine. Topical application of arbutin inhibits the production of melanin with minimal systemic absorption.Arbutin is used as a stabilizer for color photographs, diuretics, anti-infectives for the urinary system, and as a skin-lightening agent. Arbutin has similar effects as hydroquinone, inhibiting melanin formation.
Bearberry extract is used in skin lightening treatments designed for long term and regular use. An active agent in brands of skin lightening preparations, it is more expensive than traditional skin lightening ingredients like hydroquinone, which is now banned in many countries. In vitro studies of human melanocytes exposed to arbutin at concentrations below 300 μg/mL reported decreased tyrosinase activity and melanin content with little evidence of cytotoxicity.
Reducing pigmentation in the skin
Treating dark patches from sun exposure, freckles, liver spots and age spots
Using as a stabilizer for color photographs, diuretics, anti-infectives for the urinary system
Inhibiting melanin formation
Benefits
In topical formulations, the effects of arbutin are localized and dose-dependent, which provides control in managing the extent of skin lightening. Products containing arbutin can be used according to the severity of hyperpigmentation, and lower doses and reduced frequency can be employed to fine-tune skin tone. Since arbutin has limited penetration and little to no systemic absorption, use of arbutin-containing products can be stopped to allow normalized skin cells to grow (without overstimulated melanin).
Risks
Arbutin is glucosylated hydroquinone, and may carry similar cancer risks, although there are also claims that arbutin reduces cancer risk. The German Institute of Food Research inPotsdam found that intestinal bacteria can transform arbutin into hydroquinone, which creates an environment favorable for intestinal cancer.
Considerations
Topical use of arbutin is considered to be safe and effective. Since arbutin is included in various skin products, consideration regarding the effects of the other ingredients is recommended. Prolonged use of arbutin may produce uneven pigmentation such as patches of skin with no pigmentation because its effect is localized.
Audited Supplier 
){kind=link}
){kind=link}