Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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The Inhibitory Effect of Quercetin on the Agonist-Induced Regulation of Vascular Contractility

  • Je, Hyun-Dong (Department of Pharmacology, College of Pharmacy, Catholic University of Daegu) ;
  • Jeong, Ji-Hoon (Department of Pharmacology, College of Medicine, Chung-Ang University) ;
  • La, Hyen-Oh (Department of Pharmacology, College of Medicine, The Catholic University of Korea)
  • Received : 2011.04.26
  • Accepted : 2011.07.06
  • Published : 2011.10.30
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Abstract

The present study was undertaken to investigate the influence of quercetin on vascular smooth muscle contractility and to determine the mechanism involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Quercetin at a low concentration (0.01-0.03 mM) directly and more significantly relaxed fluoride or thromboxane $A_2$-induced vascular contraction than phorbol ester-induced contraction suggesting as a possible anti-hypertensive on the agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, quercetin more significantly inhibited thromboxane $A_2$-induced increases in pMYPT1 levels than phorbol ester-induced increases. It also more significantly inhibited thromboxane $A_2$-induced increases in pMYPT1 levels than pERK1/2 levels suggesting the mechanism involving the primarily inhibition of Rho-kinase activity and the subsequent phosphorylation of MYPT1. This study provides evidence regarding the mechanism underlying the relaxation effect of quercetin on agonist-induced vascular contraction regardless of endothelial function.

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References

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