The structure-activity relationship between oxycoumarin derivatives showing inhibitory effects on iNOS in mouse macrophage RAW264.7 cells

Tomonori Nakamura, Naoko Kodama, Manabu Oda, Shizuko Tsuchiya, Yu Arai, Takuya Kumamoto, Tsutomu Ishikawa, Koichi Ueno, Shingo Yano

研究成果: Article査読

30 被引用数 (Scopus)

抄録

We have investigated the structure-activity relationship between 63 natural oxycoumarin derivatives and their effects on the expression of inducible-nitric oxide synthase (iNOS) induced by lipopolysaccharide. The protein expression of iNOS was screened by Western blot analysis, and four 5,7-dimethoxycoumarins were selected as potent inhibitors of iNOS expression. In terms of structural specificity, the methoxyl group on C-5 and C-7 and the short alkyl chain (1-5 carbons) on C-6 may be essential for the potent activities. These compounds also showed inhibitory effects on nitric oxide generation and mRNA expression of inflammatory mediators, namely, iNOS and COX-2. Interestingly, the inhibitory effect on mRNA expression was specific for iNOS and was not detected for neuronal NOS. It is expected that these compounds will show anti-inflammatory activities via inhibition of the expressions of iNOS and COX-2.

本文言語English
ページ(範囲)15-20
ページ数6
ジャーナルJournal of Natural Medicines
63
1
DOI
出版ステータスPublished - 2009 1月 1
外部発表はい

ASJC Scopus subject areas

  • 薬科学
  • 創薬
  • 補完代替医療
  • 有機化学

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