Vasorelaxation Effect of Estrone Derivate EA204 in Rabbit Aorta. (14th April 2016)

• Record Type: Journal Article
• Authors: Li, Juan; Li, Wei-Qi; Yao, Yao
• Other Names: Cano Antonio Academic Editor.
• Is Part Of: Scientifica. Volume 2016(2016)
• Publication Date: 2016-04-14
• Subjects: Life sciences -- Periodicals; Biology -- Periodicals; Medicine -- Periodicals; Biological Science Disciplines; Medicine; Biology; Life sciences; Medicine; Periodicals; Electronic journals; Periodicals; 500
• DOI: 10.1155/2016/7405797
• Languages: English
• ISSNs: 2090-908X

Abstract

Abstract : Estrogen and its derivatives exert vascular protective effects, but the underlying mechanisms remain to be studied fully. Objective . To investigate the vasorelaxation effect and related mechanisms of an estrone derivate EA204[3-(2-piperidin-1-yl)-ethoxy-estra-1, 3, 5 (10)-trien-17-one] on isolated arterial preparation from rabbit thoracic aorta. Methods . Aortic rings from rabbit thoracic aorta were prepared and held in small organ bath filled with Krebs solution; tension change was recorded by a multichannel physiological signal collection and handling system. Results . EA204 (10 −5 to 10 −3 M) induced a concentration-dependent relaxation of aortic rings with endothelium and without endothelium. In denuded arterial preparations, EA204 had a potent relaxing effect on isolated arterial preparations contracted with phenylephrine, norepinephrine, and high-K + solution or BaCl2 . Mechanism study indicates that EA204 relaxes aortic rings by inhibiting Ca 2+ channels (both receptor-operating Ca 2+ channels and the voltage-dependent Ca 2+ channels were involved) to decrease extracellular Ca 2+ influx and intracellular Ca 2+ release. EA204 is different from verapamil, which is a noncompetitive inhibitor of Ca 2+ channels. In addition, K + channels opening may contribute to this vasorelaxation effect. Conclusion . EA204 had a potent endothelium-independent relaxing effect on isolated arterial preparation by inhibiting Ca 2+ channels and opening K + channels. The results suggest that EA204 is a potential compound for treatment of cardiovascular diseases in postmenopausal women.