Inhibitory Effects of (2 ' R)-2 ',3 '-dihydro-2 '-(1-hydroxy-1-methylethyl)-2,6 '-bibenzofuran-6,4 '-diol on Mushroom Tyrosinase and Melanogenesis in B16-F10 Melanoma Cells

摘要

(2 ' R)-2 ',3 '-Dihydro-2 '-(1-hydroxy-1-methylethyl)-2,6 '-bibenzofuran-6,4 '-diol (DHMB) is a natural compound extracted from Morus notabilis. It was found that DHMB acts as a competitive inhibitor against mushroom tyrosinase with a Ki value of 14.77 mu M. Docking results further indicated that it could form strong interactions with one copper ion with a distance of 2.7 angstrom, suggesting the mechanism of inhibition might be due to chelating copper ions in the active site. Furthermore, melanin production in B16-F10 murine melanoma cells was significantly inhibited by DHMB in a concentration-dependent manner without cytotoxicity. The results of western blotting also showed that DHMB decreased 3-isobuty-1-methxlzanthine-induced mature tyrosinase expression. Taken together, these findings indicated that DHMB may be a new promising pigmentation-altering agent for agriculture, cosmetic, and therapeutic applications. Copyright (c) 2015 John Wiley & Sons, Ltd.