Inhibitory effects of arbutin on melanin biosynthesis of alpha-melanocyte stimulating hormone-induced hyperpigmentation in cultured brownish guinea pig skin tissues

Arch Pharm Res. 2009 Mar;32(3):367-73. doi: 10.1007/s12272-009-1309-8. Epub 2009 Apr 23.


Arbutin has been used as a whitening agent in cosmetic products. Melanin, the major pigment that gives color to skin, may be over-produced with sun exposure or in conditions such as melasma or hyperpigmentary diseases. Tyrosinase is a key enzyme that catalyzes melanin synthesis in melanocytes; therefore, inhibitors of the tyrosinase enzyme could be used for cosmetic skin whitening. A recent study has reported that arbutin decreases melanin biosynthesis through the inhibition of tyrosinase activity. However, this inhibitory mechanism of arbutin was not sufficiently demonstrated in skin tissue models. We found that arbutin both inhibits melanin production in B16 cells induced with alpha-MSH and decreases tyrosinase activity in a cell-free system. Furthermore, the hyperpigmentation effects of alpha-MSH were abrogated by the addition of arbutin to brownish guinea pig and human skin tissues. These results suggest that arbutin may be a useful agent for skin whitening.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Agaricales / enzymology
  • Animals
  • Arbutin / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cosmetics / pharmacology*
  • Dermatologic Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology
  • Female
  • Guinea Pigs
  • Humans
  • Hyperpigmentation / drug therapy*
  • Hyperpigmentation / metabolism
  • Hyperpigmentation / physiopathology
  • Melanins / biosynthesis*
  • Melanoma, Experimental / enzymology
  • Melanoma, Experimental / metabolism*
  • Middle Aged
  • Monophenol Monooxygenase / metabolism
  • Organ Culture Techniques
  • Skin / drug effects*
  • Skin / enzymology
  • Skin / metabolism
  • Skin Pigmentation / drug effects*
  • alpha-MSH / metabolism*


  • Cosmetics
  • Dermatologic Agents
  • Enzyme Inhibitors
  • Melanins
  • alpha-MSH
  • Arbutin
  • Monophenol Monooxygenase