PHARMACOLOGICAL ANALYSIS OF THE METHANOLIC EXTRACT AND SOROCEIN-A, A NEW DIELS-ALDER COMPOUND ISOLATED FROM THE ROOTS OF SOROCEA-BONPLANDII BAILON IN THE ISOLATED RAT UTERUS AND GUINEA-PIG ILEUM

被引:9
作者
CALIXTO, JB
MESSANA, I
DELLAMONACHE, F
FERRARI, F
BISOGNIN, T
YUNES, RA
机构
[1] UNIV FED SANTA CATARINA, DEPT FARMACOL, BR-88049 FLORIANOPOLIS, SC, BRAZIL
[2] UNIV CATTOLICA S CUORE, CNR, IST CHIM RECETTORI & MOLEC BIOLOGICAMENTE ATT, I-00168 ROME, ITALY
[3] UNIV FED SANTA CATARINA, DEPT QUIM, BR-88049 FLORIANOPOLIS, SC, BRAZIL
来源
GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1993年 / 24卷 / 04期
关键词
D O I
10.1016/0306-3623(93)90177-Y
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. This study examines the effects of methanolic extract (ME) and its main constituent, sorocein A, isolated from the roots of Sorocea bonplandii on agonist-induced contractions in the rat uterus (RU) and in the guinea pig ileum (GPI) in vitro. 2. ME (25-100 mug/ml), added to RU for 20 min, caused a graded and parallel shift to the right of bradykinin (BK)-mediated contractions with an apparent pA2 value (-log g/ml) of 5.0. ME caused a rightward shift of the acetylcholine (ACh) and oxytocin-induced contractions associated with a marked depression of their maximal responses. 3. In GPI, ME produced a non-competitive antagonism against BK-induced contraction, while responses to ACh and histamine were shifted to the right in a graded fashion, yielding pA2 values (g/ml) of 5 in both cases. 4. The purified compound sorocein A (15-60 muM) caused a parallel and graded rightward displacement of BK and ACh concentration-response curves in RU with pA2 values (molar basis) of 4.9 and 5.2. 5. Sorocein A also dose-dependently shifted to the right ACh and histamine-mediated contractions in GPI, yielding pA2 values of 5.1 and 4.8, respectively. 6. However, sorocein A antagonized in a non-competitive manner BK-induced contraction in GPI, characterized by a graded displacement to the right of the dose-response curve, and progressive depression of the maximal contraction.
引用
收藏
页码:983 / 989
页数:7
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