Depigmenting Activity and Low Cytotoxicity of Alkoxy Benzoates or Alkoxy Cinnamte in Cultured Melanocytes

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  • Kang Hak Hee
    Department of Chemical Engineering, College of Engineering, Hanyang University
  • Rho Ho Sik
    R&D Center, Amore-Pacific Corporation
  • Hwang Jae Sung
    R&D Center, Amore-Pacific Corporation
  • Oh Seong-Geon
    Department of Chemical Engineering, College of Engineering, Hanyang University

書誌事項

公開日
2003
資源種別
journal article
DOI
  • 10.1248/cpb.51.1085
公開者
公益社団法人 日本薬学会

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説明

To obtain effective and safe topical depigmenting agents, we synthesized hydroxybenzoates, alkoxybenzoates, and 3,4,5-trimethoxycinnamate containing a thymol moiety and screened then for high-level inhibitory activity against melanin synthesis in cultured melanocytes. Eight compounds were tested for their depigmenting effect and cytotoxicity using a murine melanocyte cell line. We found that 3,4,5-trialkoxybenzoates and 3,4,5-trimethoxycinnamate, synthesized by conjugating 3,4,5-trialkoxybenzoic acids and 3,4,5-trimethoxycinnmic acid with thymol, showed a potent depigmenting effect and low cytotoxicity. Compound 4h, 5-methyl-2-(methylethyl)phenyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate, showed the most potent depigmenting effect (IC50=10 μM) with low cytotoxicity (IC50=200 μM).

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