冬凌草甲素对β-肾上腺素受体及腺苷酸环化酶活性的影响  

EFFECT OF ORIDONIN ON BINDING CAPACITY OF β-ADRENERGIC RECEPTOR AND ACTIVITY OF ADENYLATE CYCLASE

作　　者：李琦[1] 陈正[1] 

机构地区：[1]白求恩医科大学药理学教研室

出　　处：《白求恩医科大学学报》1991年第2期152-155,共4页Journal of Norman Bethune University of Medical Science

摘　　要：本研究采用放射性配体结合分析法和腺苷酸环化酶(AC)活性测定,观察了冬凌草甲素(Oridonin)对大鼠外周血淋巴细胞β受体的结合作用和北京鸭虹细胞膜中AC活性的影响。结果表明,Oridonin和普萘洛尔(Propranolol)一样能与标记配基竞争与β受体结合,其IC_(50)分别为6.7×10^(-5)mol/L,6.0×10^(-8)mol/L。KI值分别为1.9×10^(-5)mol/L,1.7×10^(-8)mol/L。阻断肾上腺素对膜制剂中AC活性的激动作用,从而证明Oridonin是一种较弱的β受体拮抗剂。In this experiment, we discussed the effect of Oridonin on the radioligand binding capacity to lymphocytes in rats and the activity of adenylate cyclase of Beijing duck.The results showed that both Oridonin and Propranolol inhibited the specific binding of[3H]-DHA with beta-receptor. Their apparent equilibrium dissociation constants were 1. 9 × 10-5mol/L and 1.7 × 10-8mol/L respectively.The increased activity of adenylate cyclase caused by adrenaline was completely abolished when the erythrocytes membranes containing adenylate cyclase were preincubated with Oridonin.These results demonstrate that Oridonin is a weaker beta-receptor blocking agent.

关 键 词：冬凌草 冬凌草甲素 肾上腺素受体 

分 类 号：R282.710.5[医药卫生—中药学]