环维黄杨星D对大鼠胸主动脉非内皮依赖性舒血管作用及机制研究  

Study on the endothelium-independent vasorelaxant effects of cyclovirobuxine D in rat thoracic aorta rings

作　　者：沈俊岭[1,2] 余海滨[1] 李夏寅[3] 任周新[4] 刘卫红[1] 崔琳[1] 

机构地区：[1]河南中医药大学第一附属医院,郑州450000 [2]河南省病毒性疾病中医药防治重点实验室,郑州450000 [3]中山大学附属第一医院,广州510080 [4]河南中医药大学,郑州450008

出　　处：《中药药理与临床》2017年第1期70-74,共5页Pharmacology and Clinics of Chinese Materia Medica

基　　金：河南省教育厅科技攻关项目(2011A360022);河南中医学院科研苗圃工程项目(MP2013-22)

摘　　要：目的:研究环维黄杨星D对大鼠胸主动脉去内皮血管环的舒张作用并探讨其机制。方法:采用氯化钾(KCl)或去氧肾上腺素(PE)预收缩血管,观察环维黄杨星D(10~600μmol/L)对大鼠胸主动脉去内皮血管的舒张作用;血管与600μmol/L环维黄杨星D预孵育后,观察其对KCl或PE收缩血管作用的影响;观察环维黄杨星D对不同钾离子通道阻断剂的血管反应性的影响;观察环维黄杨星D对CaCl_2收缩去内皮血管环的作用以及对PE产生的瞬时性收缩和加入CaCl_2后的持续性收缩的作用。结果:在给药浓度范围内(10~600μmol/L),环维黄杨星D能非内皮依赖性舒张由KCl和PE预收缩的大鼠胸主动脉血管环;600μmol/L环维黄杨星D与血管预孵育亦可明显抑制KCl或PE诱导的血管收缩;4-AP、Gly或TEA与血管环预孵育后,对600μmol/L环维黄杨星D舒张PE预收缩血管环的作用均没有影响;不同浓度(100、300和600μmol/L)的环维黄杨星D与血管环在无钙K-H液中预处理后,可以剂量依赖地抑制CaCl_2的浓度-效应曲线;300μmol/L环维黄杨星D与血管环在无钙K-H液中预处理后,可以显著抑制PE产生的瞬时性收缩以及加入CaCl_2后的持续性收缩。结论:环维黄杨星D对大鼠离体胸主动脉去内皮血管的舒张作用呈剂量依赖性,其对血管的舒张作用机制可能不涉及钾离子通道的活化,抑制血管平滑肌细胞的外钙内流和内钙释放作用可能参与了环维黄杨星D的舒血管机制。Objective： To observe the vasorelaxant effects of cyclovirobuxine D in isolated rat thoracic aorta rings without endothelium and to investigate the probable mechanism.Method： The vascular relaxing effect of cyclovirobuxine D at concentration range from 10 to 600 μmol/L on potassium chloride（ KCl） or phenylephrine（ PE）-precontracted aorta rings were observed.KCl or PE-induced contraction was also recorded after the aorta rings were preincubated with cyclovirobuxine D at the concentration of 600 μmol/L.When the aortic rings were in incubated with different potassium channel inhibitors,the effect of cyclovirobuxine D on aortic rings was examined and investigated.The effect of cyclovirobuxine D on the contraction of CaCl2 and the phasic or tonic contraction were observed too.Results： To KCl or PE-precontracted aorta rings,cyclovirobuxine D showed dose-dependent vasorelaxant effect at the given range of concentrations（ 10 600 μmol/L） on the rings preconstricted by KCl or PE in non-endothelium manner.Additionally,cyclovirobuxine D at the concentration of 600 μmol/L preincubation could inhibit KCl or PE-induced contraction,while 4-AP,Gly or TEA showed little effects on the vasodilation of cyclovirobuxine D.When cyclovirobuxine D at various concentration of 100 or 300 and 600 μmol/L preincubated in the K-H solution without calcium,concentration-effect curves of CaCl2 were suppressed dose-dependently; in addition,phasic and tonic contraction induced by PE and followed by the CaCl2 was significantly inhibited by cyclovirobuxine D at the concentration of 300 μmol/L.Conclusion： Cyclovirobuxine D showed effect on relaxation of rat isolated thoracic arterial rings in a dose-dependent manner,the relaxant effect may not be related to the potassium channel.Extracellular calcium influx and intracellular calcium release function of vascular smooth muscle cell may be involved in the vasorelaxation mechanism of cyclovirobuxine D.

关 键 词：环维黄杨星D 胸主动脉 去内皮 血管舒张 外钙内流 内钙释放 

分 类 号：R285.5[医药卫生—中药学]