The Inhibitory Effect of Shikonin on the Agonist-Induced Regulation of Vascular Contractility.
10.4062/biomolther.2014.148
- Author:
Hyun Dong JE
1
;
Hyeong Dong KIM
;
Hyen Oh LA
Author Information
1. Department of Pharmacology, College of Pharmacy, Catholic University of Daegu, Gyeongbuk 712-702, Republic of Korea.
- Publication Type:Original Article
- Keywords:
ERK1/2;
Fluoride;
MYPT1;
Phorbol ester;
Rho-kinase;
Shikonin
- MeSH:
Animals;
Fluorides;
Humans;
Isometric Contraction;
Lithospermum;
Male;
Muscle, Smooth, Vascular;
Nitric Oxide;
Phosphorylation;
Rats;
Relaxation;
rho-Associated Kinases
- From:Biomolecules & Therapeutics
2015;23(3):233-237
- CountryRepublic of Korea
- Language:English
-
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.
