Biomol Ther.  2014 Mar;22(2):100-105.

The Inhibitory Effect of Apigenin on the Agonist-Induced Regulation of Vascular Contractility via Calcium Desensitization-Related Pathways

• Je HD
• Kim HD
• La HO

Abstract

Apigenin, 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 apigenin 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. Apigenin significantly relaxed fluoride-, thromboxane A2 mimetic- or phorbol ester-induced vascular contraction, which suggests that apigenin could be an anti-hypertensive that reduces agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, apigenin significantly inhibited fluoride-induced increases in pMYPT1 levels and phorbol ester-induced increases in pERK1/2 levels, which suggests the mechanism involving the inhibition of Rho-kinase and MEK activity and the subsequent phosphorylation of MYPT1 and ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of apigenin on agonist-induced vascular contraction regardless of endothelial function.

Keyword

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

MeSH Terms

Animals
Apigenin*
Calcium*
Fluorides
Fruit
Humans
Isometric Contraction
Male
Muscle, Smooth, Vascular
Nitric Oxide
Phosphorylation
Rats
Relaxation
rho-Associated Kinases
Thromboxane A2
Vegetables
Apigenin
Calcium
Fluorides
Nitric Oxide
Thromboxane A2
rho-Associated Kinases