Biomol Ther.  2015 May;23(3):233-237. 10.4062/biomolther.2014.148.

The Inhibitory Effect of Shikonin on the Agonist-Induced Regulation of Vascular Contractility

• Je HD
• Kim HD
• La HO

• KMID: 2380332
• DOI: http://doi.org/10.4062/biomolther.2014.148

Abstract

Shikonin, a natural flavonoid found in the roots of Lithospermum erythrorhizon, has been shown to possess many biological functions. The present study was undertaken to investigate the influence of shikonin 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. Shikonin 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, shikonin 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 the inhibition of MEK activity and the subsequent phosphorylation of ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of shikonin on agonist-induced vascular contraction regardless of endothelial function.

Keyword

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

MeSH Terms

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