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Abstract

Arbutin: mechanism of its depigmenting action in human melanocyte culture.

K Maeda and M Fukuda
Journal of Pharmacology and Experimental Therapeutics February 1996, 276 (2) 765-769;
K Maeda
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M Fukuda
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Abstract

Arbutin, a naturally occurring beta-D-glucopyranoside of hydroquinone, is effective in the topical treatment of various cutaneous hyperpigmentations characterized by hyperactive melanocyte function. We examined the mechanism of its depigmenting action in human melanocyte cultures. Arbutin inhibited the tyrosinase activity of cultured human melanocytes at noncytotoxic concentrations. It did not affect the expression of tyrosinase mRNA. Melanin production was inhibited significantly by arbutin, as determined by measuring eumelanin radicals with an electron spin resonance spectrometer. The study of the kinetics and mechanism for inhibition of tyrosinase confirms the reversibility of arbutin as a competitive inhibitor of this enzyme. The utilization of L-tyrosine or L-dopa as the substrate suggests a mechanism involving competition with arbutin for the L-tyrosine binding site at the active site of tyrosinase. These results suggest that the depigmenting mechanism of arbutin in humans involves inhibition of melanosomal tyrosinase activity, rather than suppression of the expression and synthesis of tyrosinase.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 276, Issue 2
1 Feb 1996
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Abstract

Arbutin: mechanism of its depigmenting action in human melanocyte culture.

K Maeda and M Fukuda
Journal of Pharmacology and Experimental Therapeutics February 1, 1996, 276 (2) 765-769;

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Abstract

Arbutin: mechanism of its depigmenting action in human melanocyte culture.

K Maeda and M Fukuda
Journal of Pharmacology and Experimental Therapeutics February 1, 1996, 276 (2) 765-769;
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