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.
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 micrograms/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 microM) 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.
Calixto
J B
JB
Departmento de Farmacologia, Universidade Federal de Santa Catarina, Brazil.
Messana
I
I
Della Monache
F
F
Ferrari
F
F
Bisognin
T
T
Yunes
R A
RA
D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D001920:Bradykinin / Q000494:pharmacology; D002839:Chromans / Q000494:pharmacology*; D005260:Female; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects*; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D018377:Neurotransmitter Agents / Q000037:antagonists & inhibitors / Q000494:pharmacology; D010121:Oxytocin / Q000494:pharmacology; D010936:Plant Extracts / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D014590:Uterine Contraction / Q000187:drug effects*
D002839:Chromans; D018377:Neurotransmitter Agents; D010936:Plant Extracts; C084182:sorocein A; D010121:Oxytocin; D006632:Histamine; D000109:Acetylcholine; D001920:Bradykinin