Inhibitory Effect of 2,4,2',4'-Tetrahydroxy-3-(3-methyl-2-butenyl)-chalcone on Tyrosinase Activity and Melanin Biosynthesis(Pharmacology)
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概要
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2,4,2',4'-Tetrahydroxy-3-(3-methyl-2-butenyl)-chalcone (TMBC), a naturally occurring compound from Morus nigra, modulated melanogenesis by inhibiting tyrosinase. TMBC inhibited the L-dopa oxidase activity of mushroom tyrosinase with an IC_<50> value of 0.95±0.04μM, which was more potent than kojic acid (IC_<50>=24.88±1.13μM), a well-known tyrosinase inhibitor. The kinetic studies of tyrosinase inhibition revealed that TMBC acts as a competitive inhibitor of mushroom tyrosinase with L-dopa as the substrate. Furthermore, TMBC effectively inhibited both cellular tyrosinase activity and melanin biosynthesis in B16 melanoma cells without significant cytotoxicity. The inhibitory effect of TMBC on melanogenesis was attributed to the direct inhibition of tyrosinase activity, rather than the suppression of tyrosinase gene expression. These results indicated that TMBC may be a new promising pigmentation-altering agent for cosmetic or therapeutic applications.
- 公益社団法人日本薬学会の論文
- 2009-01-01
著者
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Hu Xiao
Department Of Physics Faculty Of Science University Of Tokyo
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Wang Heyao
Shanghai Institute Of Materia Medica Chinese Academy Of Science
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Zhang Xiaodong
Shanghai Institute Of Materia Medica Chinese Academy Of Science
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HOU Aijun
Department of Pharmacology, School of Pharmacy, Fudan University
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Hou Aijun
Department Of Pharmacology School Of Pharmacy Fudan University
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Hu Xiao
Department Of Pharmacology School Of Pharmacy Fudan University
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Hu Xiao
Department Of Electrical Engineering University Of Saskatchewan
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