Biomol Ther.  2016 Jan;24(1):57-61. 10.4062/biomolther.2015.104.

Endothelium-Independent Effect of Fisetin on the Agonist-Induced Regulation of Vascular Contractility

• Je HD
• Sohn UD
• La HO

• KMID: 2170541
• DOI: http://doi.org/10.4062/biomolther.2015.104

Abstract

Fisetin, a natural flavonoid found in a variety of vegetables and fruits, has been shown to possess many biological functions. The present study was undertaken to investigate the influence of fisetin 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. Fisetin significantly relaxed fluoride-, thromboxane A2- or phorbol ester-induced vascular contraction suggesting as a possible anti-hypertensive on the agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, fisetin significantly inhibited fluoride-induced increases in pMYPT1 levels and phorbol ester-induced increases in pERK1/2 levels suggesting the mechanism involving the inhibition of Rho-kinase activity and the subsequent phosphorylation of MYPT1 and MEK activity and the subsequent phosphorylation of ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of fisetin on agonist-induced vascular contraction regardless of endothelial function.

Keyword

ERK1/2; Fisetin; Fluoride; MYPT1; Phorbol ester; Rho-kinase

MeSH Terms

Animals
Fluorides
Fruit
Humans
Isometric Contraction
Male
Muscle, Smooth, Vascular
Nitric Oxide
Phosphorylation
Rats
Relaxation
rho-Associated Kinases
Vegetables
Fluorides
Nitric Oxide
rho-Associated Kinases