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KMID : 0043320150380040505
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Archives of Pharmacal Research
2015 Volume.38 No. 4 p.505 ~ p.511
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Inhibition of melanogenesis by 2-[4-(5-chlorobenzo[d]thiazol-2-yl)phenoxy]-2-methylpropanoic acid (MHY908)
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Park Min-Hi
Kim Seong-Jin
Jeong Hyoung-Oh
Moon Kyoung-Mi
Son Su-Jin
Kim Dae-Hyun
Kim Hye-Rim
Kim Min-Jo
Yun Hwi-Young
Chun Pu-Soon
Je Nam-Kyung
Yokozawa Takako
Moon Hyung-Ryong
Chung Hae-Young
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Abstract
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Tyrosinase inhibitors might have potential use in cosmetic and medicinal products for the prevention of pigmentation disorders. However, only a few inhibitors are currently used due to their cytotoxicity, and lack of selectivity and stability. In this study, we synthesized several tyrosinase inhibitors and investigated their activity. To investigate the action of 2-[4-(5-chlorobenzo[d]thiazol-2-yl)phenoxy]-2-methylpropanoic acid (MHY908) specifically in the inhibition of melanogenesis, a mushroom tyrosinase activity assay was performed. We confirmed the inhibitory effect of MHY908 at various melanin concentrations using α-MSH-induced melanoma cells. Our results indicate that MHY908 potently inhibited mushroom tyrosinase activity (IC50 = 8.19 μM) in a dose-dependent manner. Through a docking simulation, we also analyzed its binding mode to inhibit tyrosinase activity. MHY908 also decreased melanin synthesis without inducing cytotoxicity. These results suggest that MHY908 is a good candidate for prevention and treatment of pigmentation disorders.
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KEYWORD
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MHY908, Skin, Melanogenesis, Tyrosinase inhibitor
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