RRC ID 19365
著者 Nakamura T, Kodama N, Oda M, Tsuchiya S, Arai Y, Kumamoto T, Ishikawa T, Ueno K, Yano S.
タイトル The structure-activity relationship between oxycoumarin derivatives showing inhibitory effects on iNOS in mouse macrophage RAW264.7 cells.
ジャーナル J Nat Med
Abstract 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.
巻・号 63(1)
ページ 15-20
公開日 2009-1-1
DOI 10.1007/s11418-008-0268-6
PMID 18607531
MeSH Animals Blotting, Western Cell Line Coumarins / chemistry Coumarins / pharmacology* Lipopolysaccharides / pharmacology Macrophages / cytology Macrophages / drug effects* Macrophages / enzymology Mice Molecular Structure Nitric Oxide / metabolism Nitric Oxide Synthase Type II / antagonists & inhibitors* Nitric Oxide Synthase Type II / genetics Nitric Oxide Synthase Type II / metabolism Reverse Transcriptase Polymerase Chain Reaction Structure-Activity Relationship
IF 2.055
引用数 30
WOS 分野 PHARMACOLOGY & PHARMACY CHEMISTRY, MEDICINAL
リソース情報
ヒト・動物細胞 RAW 264(RCB0535)