2011•Chinese Journal of New Drugs and Clinical RemediesRequires access

Vasodilation effect of quercetin on rat thoracic aorta and its mechanisms

Yan Zhao, Bai-Nian Chen

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Abstract

AIM To investigate the vasodilation effect and the related mechanisms of quercetin. METHODS Tension was measured to evaluate the vasodilation effect of quercetin on rat endothelium-intact and endothelium-denuded thoracic aorta rings.The nitric oxide synthase inhibitor N~ω-nitro-L-arginine methyl ester (L-NAME),guanylyl cyclase inhibitor methylene blue,cyclooxygenase inhibitor indomethacin,calciumactivated potassium channel blocker tetraethyl ammonium(TEA),ATP-sensitive potassium channel blocker glibencla- mide and voltage-dependent potassium channel blocker 4-aminopyridine(4-AP) were used to illustrate the mechanisms of vasodilation effect of quercetin.RESULTS Quercetin(1,3,10,30,100,300μmol·L~(-1)) relaxed aortic rings pre-contracted with norepinephrine(NE,1μmol·L~(-1)) or KCl(80 mmol-L1).Pretreatment with quercetin noncompetitively inhibited contractile responses of aortas to NE or KCl.The vasorelaxant effect of quercetin did not rely on intact endothelia(P0.05).Pretreatment with L-NAME(100μmol·L~(-1)) significantly reduced the quercetin-induced vasodilation(P0.05).However,methylene blue(10μmol·L~(-1)) and indomethacin (5μmol·L~(-1)) showed no significant inhibit effects(P0.05).In endothelium-denuded rings,TEA (5 mmol·L~(-1)) significantly attenuated the vasorelaxant effect of quercetin,while glibenclamide(10μol·L~(-1)) and 4-AP(100μmol·L~(-1)) had no impact on it(P0.05).CONCLUSION The results suggested that quercetin induced relaxation in rat aortic rings through an endothelium-independent manner by blockade of Ca~(2+) channels.The opening of calcium-activated K~+ channels in vascular smooth muscle cells might also be one of the mechanisms.

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AIM To investigate the vasodilation effect and the related mechanisms of quercetin. METHODS Tension was measured to evaluate the vasodilation effect of quercetin on rat endothelium-intact and endothelium-denuded thoracic aorta rings.The nitric oxide synthase inhibitor N~ω-nitro-L-arginine methyl ester (L-NAME),guanylyl cyclase inhibitor methylene blue,cyclooxygenase inhibitor indomethacin,calciumactivated potassium channel blocker tetraethyl ammonium(TEA),ATP-sensitive potassium channel blocker glibencla- mide and voltage-dependent potassium channel blocker 4-aminopyridine(4-AP) were used to illustrate the mechanisms of vasodilation effect of quercetin.RESULTS Quercetin(1,3,10,30,100,300μmol·L~(-1)) relaxed aortic rings pre-contracted with norepinephrine(NE,1μmol·L~(-1)) or KCl(80 mmol-L1).Pretreatment with quercetin noncompetitively inhibited contractile responses of aortas to NE or KCl.The vasorelaxant effect of quercetin did not rely on intact endothelia(P0.05).Pretreatment with L-NAME(100μmol·L~(-1)) significantly reduced the quercetin-induced vasodilation(P0.05).However,methylene blue(10μmol·L~(-1)) and indomethacin (5μmol·L~(-1)) showed no significant inhibit effects(P0.05).In endothelium-denuded rings,TEA (5 mmol·L~(-1)) significantly attenuated the vasorelaxant effect of quercetin,while glibenclamide(10μol·L~(-1)) and 4-AP(100μmol·L~(-1)) had no impact on it(P0.05).CONCLUSION The results suggested that quercetin induced relaxation in rat aortic rings through an endothelium-independent manner by blockade of Ca~(2+) channels.The opening of calcium-activated K~+ channels in vascular smooth muscle cells might also be one of the mechanisms.

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Available abstract

AIM To investigate the vasodilation effect and the related mechanisms of quercetin. METHODS Tension was measured to evaluate the vasodilation effect of quercetin on rat endothelium-intact and endothelium-denuded thoracic aorta rings.The nitric oxide synthase inhibitor N~ω-nitro-L-arginine methyl ester (L-NAME),guanylyl cyclase inhibitor methylene blue,cyclooxygenase inhibitor indomethacin,calciumactivated potassium channel blocker tetraethyl ammonium(TEA),ATP-sensitive potassium channel blocker glibencla- mide and voltage-dependent potassium channel blocker 4-aminopyridine(4-AP) were used to illustrate the mechanisms of vasodilation effect of quercetin.RESULTS Quercetin(1,3,10,30,100,300μmol·L~(-1)) relaxed aortic rings pre-contracted with norepinephrine(NE,1μmol·L~(-1)) or KCl(80 mmol-L1).Pretreatment with quercetin noncompetitively inhibited contractile responses of aortas to NE or KCl.The vasorelaxant effect of quercetin did not rely on intact endothelia(P0.05).Pretreatment with L-NAME(100μmol·L~(-1)) significantly reduced the quercetin-induced vasodilation(P0.05).However,methylene blue(10μmol·L~(-1)) and indomethacin (5μmol·L~(-1)) showed no significant inhibit effects(P0.05).In endothelium-denuded rings,TEA (5 mmol·L~(-1)) significantly attenuated the vasorelaxant effect of quercetin,while glibenclamide(10μol·L~(-1)) and 4-AP(100μmol·L~(-1)) had no impact on it(P0.05).CONCLUSION The results suggested that quercetin induced relaxation in rat aortic rings through an endothelium-independent manner by blockade of Ca~(2+) channels.The opening of calcium-activated K~+ channels in vascular smooth muscle cells might also be one of the mechanisms.

Key concepts: Quercetin, Vasodilation, Glibenclamide, Chemistry, Potassium channel, Channel blocker, Potassium channel blocker, Methylene blue

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