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Synthesis of 2',4'-Dimethoxyflavone and Its Anti-pigmentation Effect  

Lee, Bum-Chun (R&D Center, Hanbul Cosmetics Co. Ltd.)
Sim, Gwan-Sub (R&D Center, Hanbul Cosmetics Co. Ltd.)
Kim, Jin-Hwa (R&D Center, Hanbul Cosmetics Co. Ltd.)
Kim, Ki-Ho (R&D Center, Bioland Ltd.)
Lee, Hwa-Jeong (College of Pharmacy, Chungbuk National University)
Pyo, Hyeong-Bae (R&D Center, Hanbul Cosmetics Co. Ltd.)
Publication Information
Journal of the Society of Cosmetic Scientists of Korea / v.32, no.3, 2006 , pp. 153-160 More about this Journal
Abstract
We synthesized 2',4'-dimethoxyflavone and investigated the effects on melanogenesis. To determine the effects as a whitening agent, various in uitro tests were performed such as free radical scavenging activity, melanin assay, tyrosinase activity and expression of tyrosinase, TRP-1 and TRP-2 (western blot and RT-PCR) in Bl6 melanoma cells. 2',4'-Dimethoxyflavone showed neither free radical scavenging activities against 1,1- diphenyl -2-picrylhydrazvl (DPPH) radical and inhibition of mushroom tyrosinase activity, 2',4'-dimethoxyflavone significantly inhibited melanin production in B16 melanoma cells. 2',4'-Dimethoxyflavone treatment (48h) suppressed the biosynthesis of melanin up to 27% at $5{\mu}g/mL$ and reduced tyrosinase activity up to 20% at $5{\mu}g/mL$ in B16 melanoma cells. 2',4'-Dimethoxyflavone was also able to significantly inhibit tyrosinase and TRP-1 expression in protein and mRNA level. These results suggest that 2',4'-dimethoxyflavone inhibits melanin biosynthesis at the level of enzyme activity and protein mRNA expression B16 melanoma cells. Therefore, 2',4'-dimethoxyflavone may be useful as a new whitening agent in cosmetics.
Keywords
2',4'-dimethoxyflavone; synthesis; melanogenesis; tyrosinase; TRP-1,2;
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