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

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Maeda K, Fukuda M

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

J Pharmacol Exp Ther. 1996 Feb;276(2):765-9.

PubMed ID

8632348 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drugs

Arbutin

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Arbutin	Tyrosinase	Protein	Humans	Yes	Inhibitor	Details