Calixto J B, Nicolau M, Yunes R A
Br J Pharmacol. 1985 Aug;85(4):729-31. doi: 10.1111/j.1476-5381.1985.tb11069.x.
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.
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。
