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.
Original language | English |
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Pages (from-to) | 15-20 |
Number of pages | 6 |
Journal | Journal of Natural Medicines |
Volume | 63 |
Issue number | 1 |
DOIs | |
Publication status | Published - 2009 Jan 1 |
Externally published | Yes |
Keywords
- Inducible nitric oxide synthase
- Macrophage
- Oxycoumarin
- RAW264.7
- Structure-activity relationship
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery
- Complementary and alternative medicine
- Organic Chemistry