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Topical Hypopigmenting Agents for Pigmentary Disorders and Their Mechanisms of Action

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초록

Melanin is produced in melanocytes and stored in melanosomes. In spite of its beneficial sun- protective effect,abnormal accumulation of melanin results in esthetic problems. Hydroquinone, competing with tyrosine, is a major ingredient in topical pharmacological agents. However,frequent adverse reactions are amongst its major limitation. To solve this problem, several alternatives such as arbutin, kojic acid, aloesin, and 4-n-butyl resorcinol have been developed. Herein, we classify hypopigmenting agents according to their mechanism of action; a) regulation of enzyme, which is subdivided into three categories, i)regulation of transcription and maturation of tyrosinase, ii)inhibition of tyrosinase activity, and iii) post-transcriptional control of tyrosinase; b) inhibition of melanosome transfer,and c) additional mechanisms such as regulation of the melanocyte environment and antioxidant agents.

Abstract

Melanin is produced in melanocytes and stored in melanosomes. In spite of its beneficial sun- protective effect,abnormal accumulation of melanin results in esthetic problems. Hydroquinone, competing with tyrosine, is a major ingredient in topical pharmacological agents. However,frequent adverse reactions are amongst its major limitation. To solve this problem, several alternatives such as arbutin, kojic acid, aloesin, and 4-n-butyl resorcinol have been developed. Herein, we classify hypopigmenting agents according to their mechanism of action; a) regulation of enzyme, which is subdivided into three categories, i)regulation of transcription and maturation of tyrosinase, ii)inhibition of tyrosinase activity, and iii) post-transcriptional control of tyrosinase; b) inhibition of melanosome transfer,and c) additional mechanisms such as regulation of the melanocyte environment and antioxidant agents.

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