橙皮素通过cAMP/PKA/Kv1.2通路舒张大鼠冠状动脉  

Vasorelaxing Effect of Hesperetin on Coronary Artery via Activating c AMP/PKA/Kv1. 2 Pathway in Rats

作　　者：刘宇[1] 邢国芳 张蕾[1] 霍娉婷 宋奇颖 Liu Yü;Xing Guofang;Zhang Lei;Huo Pingting;Song Qiying(Department of Pharmacology,Shanxi Medical University,Taiyuan 030001)

机构地区：[1]山西医科大学药理学教研室,太原030001

出　　处：《中药药理与临床》2020年第1期60-63,共4页Pharmacology and Clinics of Chinese Materia Medica

基　　金：国家自然科学基金项目(编号:81603111);山西省“1331工程”重点学科建设计划经费(编号:XK201708);山西医科大学博士启动基金(编号:03200707)。

摘　　要：目的:探讨橙皮素在舒张大鼠冠状动脉(RCA)中的c AMP/PKA/Kv1. 2通路机制。方法:离体血管张力法记录RCA血管张力;从RCA急性分离动脉血管平滑肌,采用膜片钳技术测定其Kv电流。结果:Kv1. 2抑制剂Charybdotoxin (Ch TX)减弱橙皮素对RCA的舒张作用,而Kv1. 5抑制剂DPO-1、Kv2. 1抑制剂Guangxitoxin和Kv7抑制剂XE991对橙皮素的血管舒张作用无显著影响。膜片钳结果为,Ch TX显著减小橙皮素引起的Kv电流净增加,而DPO-1、Guangxitoxin和XE991对橙皮素所致的Kv电流净增加无显著性影响。蛋白激酶A(PKA)抑制剂Rp-cAMP减弱橙皮素对RCA的舒张作用,同时减小橙皮素所致的Kv电流增加。结论:橙皮素对大鼠RCA的舒张作用至少部分是通过增加c AMP/PKA/Kv1. 2活性而实现的。Objective: To explore the vasorelaxing effect of hesperetin on rat coronary artery( RCA) by c AMP/PKA/Kv1. 2 pathway. Methods:The RCA vascular tension was recorded by a wire myograph in vitro. The artery smooth muscle cells were freshly isolated from RCA,then Kv currents was measured by patch clamp. Results: Kv1. 2 inhibitor charybdotoxin( Ch TX) attenuated the vasorelaxing effect of hesperetin on RCA,while Kv1. 5 inhibitor DPO-1,Kv2. 1 inhibitor Guangxitoxin and Kv7 inhibitor XE991 showed no significant effect on hesperetin vasorelaxing effect. The patch clamp results showed that,Ch TX significantly decreased the net increase of Kv currents induced by hesperetin,while Guangxitoxin and XE991 had no significant effect. Protein kinase A( PKA) inhibitor Rp-c AMP attenuated the vasorelaxing effect of hesperetin on RCA and decreased the Kv current increase induced by hesperetin. Conclusion: The relaxation effect of hesperetin on rat coronary artery may partly be activating c AMP/PKA/Kv1. 2 pathway.

关 键 词：橙皮素 冠状动脉 血管舒张 电位依赖性钾通道 环磷酸腺苷 

分 类 号：R285.5[医药卫生—中药学]