Vasorelaxant effect of FR900359 from Ardisia crenata on rat aortic artery

• Published in: Journal of natural medicines Vol. 67; no. 1; pp. 196 - 201
• Main Authors: Zaima, Kazumasa, Deguchi, Jun, Matsuno, Yosuke, Kaneda, Toshio, Hirasawa, Yusuke, Morita, Hiroshi
• Format: Journal Article
• Language: English
• Published: Japan Springer-Verlag 01-01-2013; Springer Japan
• Subjects: Animals; aorta; Aorta - drug effects; Ardisia; Ardisia - chemistry; Arteries - drug effects; Biomedical and Life Sciences; Biomedicine; calcium; Complementary & Alternative Medicine; endothelial cells; Male; Medicinal Chemistry; nitric oxide; Nitric Oxide - metabolism; Pharmacology/Toxicology; Pharmacy; Plant Sciences; Rats; Rats, Wistar; vasodilation; Vasodilator Agents - pharmacology; Vasorelaxant effect; FR900359; Rat aortic artery
• ISSN: 1340-3443; 1861-0293
• DOI: 10.1007/s11418-012-0644-0

A cyclic depsipeptide, FR900359, isolated from Ardisia crenata was evaluated for vasorelaxant effects on rat aortic arteries. FR900359 caused concentration-dependent relaxation (1 nM–10 μM) in phenylephrine-precontracted endothelium-intact aortic rings, which was inhibited by addition of L-NMMA, a NOS inhibitor. In endothelium-denuded rings, the relaxant effect of low concentrations of FR900359 was diminished, but remained at high concentrations. In endothelium-denuded rings, FR900359 at 0.1 μM significantly attenuated high-K⁺-induced contractions and completely inhibited Ca²⁺-induced contractions. These results suggest that the vasorelaxant effect of FR900359 is mediated through the increased release of NO from endothelial cells at low concentrations, and can be attributed to inhibitory effects on voltage-dependent Ca²⁺ channel- and receptor-operated Ca²⁺ channel-dependent Ca²⁺ influx at high concentrations.