Action of pregnane compounds from Mandevilla illustris against contractions induced by kinins and other oxytocics in the rat isolated uterus.
1. The effects of 5 pregnane compounds isolated from the rhizomes of Mandevilla illustris were examined against bradykinin (BK), Lysyl-bradykinin (L-BK), acetylcholine (ACh) and oxytocin (Ot)-induced contractions in the isolated uteri of the rat. 2. Compounds MI 15 and MI 18 (5-40 micrograms/ml) caused a parallel and concentration-dependent rightward displacement of BK and L-BK concentration-response curves. Compound MI 21 (2.5-10 micrograms/ml) also produced a concentration-dependent displacement to the right of the BK concentration-response curve, but reduced its maximal response. Schild analysis of these data were linear (r close to 1) and furnished the following PA2 values (as G/ml): 6.0, 5.1 and 5.9, respectively. However, the slopes were significantly higher than unity. Compounds MI 25 and MI 27 (10-40 micrograms/ml) caused little or even no effect against BK and ACh responses. 3. In addition, compounds MI 18 and MI 21 (10-40 micrograms/ml) also antagonized in a concentration-dependent manner L-BK concentration-response curves. Schild plot were linear (r close to 1) and yielded the nominal pA2 values (as G/ml) of 5.0 and 5.8, respectively, but the slopes were significantly different from one. 4. Like the results obtained previously with the crude extract from M. illustris, the purified compounds from the rhizome of this plant were not selective towards kinin action since at the same range concentrations they markedly interfered with both the sensitivities and the maximal responses caused by ACh and Ot in this preparation.
Calixto
J B
JB
Department of Pharmacology, Universidade Federal de Santa Catarina, Florianópolis, Brazil.
Brum
R L
RL
Yunes
R A
RA
D000109:Acetylcholine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001920:Bradykinin / Q000037:antagonists & inhibitors / Q000494:pharmacology; D005260:Female; D066298:In Vitro Techniques; D007609:Kallidin / Q000494:pharmacology; D007705:Kinins / Q000037:antagonists & inhibitors*; D010120:Oxytocics / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D010121:Oxytocin / Q000037:antagonists & inhibitors / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry*; D011278:Pregnanes / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D014590:Uterine Contraction / Q000187:drug effects*
D007705:Kinins; D010120:Oxytocics; D011278:Pregnanes; D007609:Kallidin; D010121:Oxytocin; D000109:Acetylcholine; D001920:Bradykinin