目的:研究毛冬青正丁醇提取物(n-butyl alcohol extractive of Ilex pubescens Hook,NAI)的扩血管作用。方法:采集内皮完整和去内皮新西兰兔离体胸主动脉环等长张力,观察NAI对正常及不同痉挛状态下动脉环张力的影响,并观察其作用与钙通道、钾通道、组胺受体、血管内皮系统的关系。结果:NAI(1.2、0.6、0.3 mg/ml)对正常状态下的内皮完整和去内皮动脉环张力无显著作用。NAI(1.2、0.6、0.3 mg/ml)显著舒张去甲肾上腺素(NE)引起的去内皮动脉环收缩,对KCl、组胺引起的去内皮动脉环收缩无显著舒张作用;NAI(1.2、0.6 mg/ml)能显著降低高钾去极化去内皮兔胸主动脉环Ca Cl2引起的最大收缩率;NAI(1.2、0.3 mg/ml)显著舒张AngⅡ引起的内皮完整动脉环收缩。NAI(0.3、0.6 mg/ml)显著舒张经L-NG-硝基精氨酸甲酯(L-NAME)预处理后NE引起的动脉环血管收缩,但对经过亚甲蓝、吲哚美辛预处理后NE引起的动脉环血管收缩无显著舒张作用。NAI(1.2、0.6、0.3 mg/ml)抑制无钙Krebs液中NE诱导的内钙释放所引起的血管收缩反应,对复钙后NE所致的血管持续收缩亦有显著抑制作用。NAI(1.2、0.6、0.3 mg/ml)显著抑制NE引起的内皮完整和去内皮动脉环收缩累积量效曲线,去除内皮后,NAI的扩血管作用显著减弱。结论:NAI对正常状态下内皮完整和去内皮动脉环张力无显著作用,NAI显著舒张NE、Ca Cl2、AngⅡ、L-NAME引起的动脉环血管收缩,对KCl、组胺、亚甲蓝、吲哚美辛引起的动脉环收缩无显著舒张作用。其扩血管作用与受体操纵性钙通道,介导内皮合成、释放一氧化氮(NO)、拮抗血管紧张素Ⅱ(AngⅡ)、抑制内钙释放和外钙内流有关,具有一定的内皮依赖性。
Objective: to investigate the vasorelaxant effect of n-Bu OH extract of the radix of Ilex pubescens Hook et Arn( NAI). Methods: The vasorelaxant activity of NAI were observed by detecting and measuring the tension force of rabbits’ endothelium-intact and-denuded thoracic aortic rings under vasodilatation and vasospasm,find out the inner connection between NAI’s effect and calcium channel,potassium channel,histamine receptors and endothelial system. Results: NAI( 0. 3,0. 6,1. 2 mg / m L) had no effect on tension force of rabbit thoracic aortic rings with or without endothelium. NAI( 0. 3,0. 6,1. 2 mg / m L) concentration-dependently inhibited the spasm induced by NE,but not by KCl and histamine; NAI( 0. 6,1. 2 mg / m L) can significantly shifted Calcium concentration-dependent contraction curves to the right and downward in high potsssium depolarization medium and decreased the maximum responses; NAI( 0. 3,1. 2 mg / m L) lowered the dose-effect curves of aortic rings of angiotensinⅡ( AngⅡ) and decreased the maximum responses; NAI( 0. 3,0. 6 mg / m L) were significantly reduced the relaxant effect of aortic rings pretreated with L-NAME,but not with MB and indometacin. NAI( 0. 3,0. 6,1. 2 mg / m L) concentrationdependently tended to inhibit the long-lasting contraction induced by addition of Ca2 +,while NAI( 0. 3,0. 6,1. 2 mg/m L) shifted NE concentration-dependent contraction curves significantly to the right and downward,and the maximum responses decrease,rather the relaxing response was significantly attenuated by removal of endothelium. Conclusion: NAI has no had no effect on tension force rabbit thoracic aortic rings under vasodilatation. NAI had obvious relaxation against the spasm of the aortic rings induced by NE,Ca Cl2,angiotensinⅡ( AngⅡ)and L-NAME,rather it had no significant vasorelaxant effect against the spasm induced by KCl,histamine,methylene blue and indometacin.Its vasorelaxant effect is related to receptor operated calcium channel,endoth