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粗制软毛曼陀罗提取物对大鼠离体子宫缓激肽作用的选择性拮抗作用。

The selective antagonism of bradykinin action on rat isolated uterus by crude Mandevilla velutina extract.

作者信息

Calixto J B, Nicolau M, Yunes R A

出版信息

Br J Pharmacol. 1985 Aug;85(4):729-31. doi: 10.1111/j.1476-5381.1985.tb11069.x.

Abstract

A crude aqueous alcoholic extract of Mandevilla velutina (Apocynaceae) rhizomes produced a concentration-dependent displacement to the right of the concentration-response curve to bradykinin (Bk) in the isolated uterus of the rat. Schild analysis of the data revealed a linear relationship (r = 0.99) and yielded a pA2 value of 3.3 + 0.08 (- log g ml-1) but the slope differed significantly from unity. The anti-Bk action was of rapid onset and was reversible upon washout. Contractions induced by acetylcholine, oxytocin, angiotensin II and BaCl2 were unaffected by the extract. This represents the first report of a selective Bk antagonist of plant origin. The isolation of the active principle(s) may result in a useful pharmacological tool for elucidating the physiological and physiopathological roles of endogenous Bk.

摘要

曼德维拉绒毛根(夹竹桃科)的粗制水醇提取物,在大鼠离体子宫中,使缓激肽(Bk)浓度-反应曲线向右产生浓度依赖性位移。对数据进行的Schild分析显示呈线性关系(r = 0.99),pA2值为3.3 + 0.08(-log g ml-1),但斜率与1有显著差异。抗Bk作用起效迅速,冲洗后可逆。乙酰胆碱、催产素、血管紧张素II和BaCl2诱导的收缩不受该提取物影响。这是关于植物来源的选择性Bk拮抗剂的首次报道。活性成分的分离可能会产生一种有用的药理学工具,用于阐明内源性Bk的生理和病理生理作用。

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