Understanding the cardioprotective effects of flavonols: discovery of relaxant flavonols without antioxidant activity

Qin, C, Chen, X, Hughes, R, Williams, S and Woodman, O 2008, 'Understanding the cardioprotective effects of flavonols: discovery of relaxant flavonols without antioxidant activity', Journal of medicinal chemistry, vol. 51, pp. 1874-1884.


Document type: Journal Article
Collection: Journal Articles

Title Understanding the cardioprotective effects of flavonols: discovery of relaxant flavonols without antioxidant activity
Author(s) Qin, C
Chen, X
Hughes, R
Williams, S
Woodman, O
Year 2008
Journal name Journal of medicinal chemistry
Volume number 51
Start page 1874
End page 1884
Total pages 11
Publisher American Chemical Society
Abstract 3?,4?-Dihydroxyflavonol (DiOHF) is a cardioprotective flavonol that can reduce injury after myocardial ischemia and reperfusion and thus is a promising small molecule for the treatment of cardiovascular disease. Like all vasoactive flavonols reported to date, DiOHF is both relaxant and antioxidant, hindering investigation of the relative contribution of each activity for the prevention of reperfusion injury. This study investigates structure-activity relationships of variations at the 3? and 4? positions of the B ring of DiOHF and vasorelaxant and antioxidant activities. Relaxation of rat isolated aortic rings precontracted with KCl revealed that the most active flavonols were those with a 4?-hydroxyl group, with the opening of potassium channels as a possible contributing mechanism. For the antioxidant activity, with the exception of DiOHF, none of the flavonols investigated were able to significantly scavenge superoxide radical, and none of the three most potent vasorelaxant flavonols could prevent oxidant-induced endothelial dysfunction. The discovery of single-acting vasorelaxant flavonols without antioxidant activity, in particular 4?-hydroxy-3?-methoxyflavonol, will assist in investigating the mechanism of flavonol-induced cardioprotection
Subject Basic Pharmacology
DOI - identifier 10.1021/jm070352h
Copyright notice © 2008 American Chemical Society.
ISSN 0022-2623
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