Effects of flavonoids on vascular smooth muscle of the isolated rat thoracic aorta

The potency, structure-activity relationship, and mechanism of vasorelaxation of a series of flavonoids, representing different subclasses (flavonols: fisetin, rutin, quercetin; flavones: chrysin, flavone, baicalein; flavanones: naringenin, naringin; isoflavones: diadzein and flavanes: epigallo cate...

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Bibliographic Details
Published in:Life sciences (1973) 2003-12, Vol.74 (5), p.603-612
Main Authors: Ajay, Machha, Gilani, Anwar-ul Hassan, Mustafa, Mohd.Rais
Format: Article
Language:English
Subjects:
Animals
Aorta, Thoracic - drug effects
Cyclooxygenase Inhibitors - pharmacology
Enzyme Inhibitors - pharmacology
Flavonoids
Flavonoids - pharmacology
In Vitro Techniques
Indomethacin - pharmacology
Male
Muscle Contraction - drug effects
Muscle Relaxation - drug effects
Muscle, Smooth, Vascular - drug effects
NG-Nitroarginine Methyl Ester - pharmacology
Nitric Oxide Synthase - antagonists & inhibitors
Nitric Oxide Synthase Type III
Phenylephrine - antagonists & inhibitors
Phenylephrine - pharmacology
Potassium - antagonists & inhibitors
Potassium - pharmacology
Rat aorta
Rats
Rats, Inbred WKY
Structure-Activity Relationship
Vasoconstrictor Agents - antagonists & inhibitors
Vasoconstrictor Agents - pharmacology
Vasorelaxant
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Summary:The potency, structure-activity relationship, and mechanism of vasorelaxation of a series of flavonoids, representing different subclasses (flavonols: fisetin, rutin, quercetin; flavones: chrysin, flavone, baicalein; flavanones: naringenin, naringin; isoflavones: diadzein and flavanes: epigallo catechin gallate), were examined in the isolated rat aorta. Most of the flavonoids tested showed concentration dependent relaxant effects against K + (80 mM) and phenylephrine (PE, 0.1 μM)-induced contractions with a greater inhibition of the responses to the α 1-adrenoceptor agonist. The relaxant effects of most of the flavonoids involve in part the release of nitric oxide and prostaglandins from the endothelium as pretreatment with L-NAME and indomethacin attenuated the responses. In addition, the relaxant action of the flavonoids includes inhibition of Ca +2 influx and release of Ca +2 from intracellular stores. A structure-activity relationship amongst the flavonoids was suggested.
ISSN:0024-3205
1879-0631
DOI:10.1016/j.lfs.2003.06.039