Open AccessTyrosinase Inhibitory Activity of a Glucosylated Hydroxystilbene in Mouse Melan-a Melanocytes
Author(s) -
Fanny M. Cheung,
Alex Wing Kwan Leung,
Wing Keung Liu,
Chun Tao
Publication year - 2014
Publication title -
journal of natural products
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.976
H-Index - 139
eISSN - 1520-6025
pISSN - 0163-3864
DOI - 10.1021/np4008798
Subject(s) - tyrosinase , endoplasmic reticulum , biochemistry , microphthalmia associated transcription factor , polygonum , chemistry , enzyme , transcription factor , non competitive inhibition , biology , microbiology and biotechnology , gene , ecology
2,3,5,4'-Tetrahydroxystilbene-2-O-β-D-glucopyranoside (1), isolated from Polygonum multiflorum, is a noncompetitive inhibitor of tyrosinase in cell-free kinetics; it reduced the Vmax values in a dose-dependent manner. Compound 1 inhibited PKA-induced melanogenesis, reduced the protein expression of tyrosinase and its transcription factor, the microphthalmia-associated transcription factor, and lowered the complex formation between tyrosinase and tyrosinase-related protein 1 (TRP-1). Immunofluorescence microscopy revealed no association of tyrosinase with the endoplasmic reticulum or lysosomes, implying the absence of a direct effect of 1 on the maturation process of the enzyme. The antimelanogenic activity of 1 is likely mediated through a noncompetitive inhibition on tyrosinase, down-regulation of the expression of melanogenic proteins, and reduction of tyrosinase/TRP-1 complex formation.