We studied the inhibitory effects of 4-hydroxyphenyl α- glucopyranoside (α-arbutin) on melanogenesis in cultured human melanoma cells, HMV-II, and in a three-dimensional cultured human skin model. α-Arbutin showed no inhibitory effect on HMV-II cell growth at a concentration below 1.0mm. Melanin synthesis in cells treated with α-arbutin at 0.5mm 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 μg of α-arbutin did not inhibit cell viability, while melanin synthesis was reduced to 40% of that in the control. These results indicate that α-arbutin is an effective and safe ingredient for skin-lightening. © 2004 Pharmaceutical Society of Japan.
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Sugimoto, K., Nishimura, T., Nomura, K., Sugimoto, K., & Kuriki, T. (2004). Inhibitory effects of α-arbutin on melanin synthesis in cultured human melanoma cells and a three-dimensional human skin model. Biological and Pharmaceutical Bulletin, 27(4), 510–514. https://doi.org/10.1248/bpb.27.510