title: 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.
abstract: (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 μM. Docking results further indicated that it could form strong interactions with one copper ion with a distance of 2.7 Å, 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.
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang Hi-Tech Park, Pudong, Shanghai, 201203, China.
authors.forename: Jing-Jie
authors.initials: JJ
authors.lastname: Zhu
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang Hi-Tech Park, Pudong, Shanghai, 201203, China.
authors.forename: Gui-Rui
authors.initials: GR
authors.lastname: Yan
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang Hi-Tech Park, Pudong, Shanghai, 201203, China.
authors.forename: Zhi-Jian
authors.initials: ZJ
authors.lastname: Xu
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, Fudan University, 826 Zhang Heng Road, Shanghai, 201203, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Hu
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang Hi-Tech Park, Pudong, Shanghai, 201203, China.
authors.forename: Gai-Hong
authors.initials: GH
authors.lastname: Wang
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang Hi-Tech Park, Pudong, Shanghai, 201203, China.
authors.forename: Ting
authors.initials: T
authors.lastname: Wang
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang Hi-Tech Park, Pudong, Shanghai, 201203, China.
authors.forename: Wei-Liang
authors.initials: WL
authors.lastname: Zhu
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, Fudan University, 826 Zhang Heng Road, Shanghai, 201203, China.
authors.forename: Ai-Jun
authors.initials: AJ
authors.lastname: Hou
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang Hi-Tech Park, Pudong, Shanghai, 201203, China.
authors.forename: He-Yao
authors.initials: HY
authors.lastname: Wang
mesh_terms: D000363:Agaricales / Q000201:enzymology*; D000818:Animals; D001572:Benzofurans / Q000737:chemistry*; D045744:Cell Line, Tumor; D000242:Cyclic AMP / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry; D008543:Melanins / Q000096:biosynthesis*; D008546:Melanoma, Experimental / Q000378:metabolism*; D051379:Mice; D062105:Molecular Docking Simulation; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*; D031625:Morus / Q000737:chemistry
chemical_list: C578234:(2'R)-2',3'-dihydro-2'-(1-hydroxy-1-methylethyl)-2,6'-bibenzofuran-6,4'-diol; D001572:Benzofurans; D004791:Enzyme Inhibitors; D008543:Melanins; D000242:Cyclic AMP; D014442:Monophenol Monooxygenase
keywords: (2′R)-2′,3′-dihydro-2′-(1-hydroxy-1-methylethyl)-2,6′-bibenzofuran-6,4′-diol; Moraceae; Morus notabilis; inhibitor; melanogenesis; tyrosinase