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Murine tyrosinase Inhibitors from Cynanchum bungei and evaluation of in vitro and in vivo depigmenting activity
Author(s) -
Ding HsiouYu,
Chang TeSheng,
Shen HungChang,
Tai Sorgan ShouKu
Publication year - 2011
Publication title -
experimental dermatology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.108
H-Index - 96
eISSN - 1600-0625
pISSN - 0906-6705
DOI - 10.1111/j.1600-0625.2011.01302.x
Subject(s) - tyrosinase , dhap , in vivo , chemistry , in vitro , arbutin , pharmacology , microbiology and biotechnology , cytotoxicity , biochemistry , enzyme , biology
Two natural acetophenone derivatives, 2,5‐dihydroxyacetophenone (2,5‐DHAP) and 2,6‐DHAP, were purified from Cynanchum bungei and identified as murine tyrosinase inhibitors. Investigation into 2,5‐DHAP showed it to be an uncompetitive inhibitor of murine tyrosinase ( K I 0.28 m m ). 2,5‐DHAP strongly inhibited both melanogenesis and cellular tyrosinase activity in vitro in 3‐isobutyl‐1‐methylxanthin ‐stimulated B16 mouse melanoma cells or in vivo in zebrafish and mouse models, but showed no cytotoxicity at the concentrations used. In B16 cells, 2,5‐DHAP inhibition was dose‐dependent and was fourfold greater than that of arbutin. 2,5‐DHAP had no effect on the expression of tyrosinase protein or mRNA, as confirmed by Western blotting and quantitative real‐time reverse transcription polymerase chain reaction, respectively. A 2% gel preparation of 2,5‐DHAP applied to the skin of mice significantly increased the average skin‐whitening index ( L value), indicating its potential use as a treatment for skin hyperpigmentation in humans.