Inhibitory effects of alpha-arbutin on melanin synthesis in cultured human melanoma cells and a three-dimensional human skin model

Biol Pharm Bull. 2004 Apr;27(4):510-4. doi: 10.1248/bpb.27.510.


We studied the inhibitory effects of 4-hydroxyphenyl alpha-glucopyranoside (alpha-arbutin) on melanogenesis in cultured human melanoma cells, HMV-II, and in a three-dimensional cultured human skin model. alpha-Arbutin showed no inhibitory effect on HMV-II cell growth at a concentration below 1.0 mM. Melanin synthesis in cells treated with alpha-arbutin at 0.5 mM decreased to 76% of that in non-treated cells. The cellular tyrosinase activity of HMV-II cells also significantly decreased, while the expression of its mRNA was not affected. Melanin synthesis in a human skin model was also evaluated by the macro- and microscopic observation of its pigmentation as well as by quantitative measurements of melanin. Treatment of the human skin model with 250 microg of alpha-arbutin did not inhibit cell viability, while melanin synthesis was reduced to 40% of that in the control. These results indicate that alpha-arbutin is an effective and safe ingredient for skin-lightening.

MeSH terms

  • Arbutin / pharmacology*
  • Cell Division / drug effects
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Melanins / antagonists & inhibitors*
  • Melanins / biosynthesis
  • Melanoma
  • Models, Biological
  • Monophenol Monooxygenase / antagonists & inhibitors
  • Monophenol Monooxygenase / biosynthesis
  • Monophenol Monooxygenase / genetics
  • Organ Culture Techniques
  • Reverse Transcriptase Polymerase Chain Reaction
  • Skin / drug effects*
  • Skin / metabolism
  • Tumor Cells, Cultured


  • Enzyme Inhibitors
  • Melanins
  • Arbutin
  • Monophenol Monooxygenase