| RRC ID |
19365
|
| Author |
Nakamura T, Kodama N, Oda M, Tsuchiya S, Arai Y, Kumamoto T, Ishikawa T, Ueno K, Yano S.
|
| Title |
The structure-activity relationship between oxycoumarin derivatives showing inhibitory effects on iNOS in mouse macrophage RAW264.7 cells.
|
| Journal |
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.
|
| Volume |
63(1)
|
| Pages |
15-20
|
| Published |
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
|
| Times Cited |
30
|
|
WOS Category
|
PHARMACOLOGY & PHARMACY
CHEMISTRY, MEDICINAL
|
| Resource |
| Human and Animal Cells |
RAW 264(RCB0535) |
