ACTION OF PREGNANE COMPOUNDS FROM MANDEVILLA-ILLUSTRIS AGAINST CONTRACTIONS INDUCED BY KININS AND OTHER OXYTOCICS IN THE RAT ISOLATED UTERUS

被引:3
作者
CALIXTO, JB [1 ]
BRUM, RL [1 ]
YUNES, RA [1 ]
机构
[1] UNIV FED SANTA CATARINA, DEPT CHEM CFM, BR-88049 FLORIANOPOLIS, SC, BRAZIL
来源
GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1991年 / 22卷 / 06期
关键词
D O I
10.1016/0306-3623(91)90579-U
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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-mu-g/ml) caused a parallel and concentration-dependent rightward displacement of BK and L-BK concentration response curves. Compound MI 21 (2.5-10-mu-g/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-mu-g/ml) caused little or even no effect against BK and ACh responses. 3. In addition. compounds MI 18 and MI 21 (10-40-mu-g/ml) also antagonized in a concentration-dependent manner L-BK concentration response curves. Schild plot were linear (r close to l) 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.
引用
收藏
页码:1071 / 1075
页数:5
相关论文
共 13 条
[1]   SOME QUANTITATIVE USES OF DRUG ANTAGONISTS [J].
ARUNLAKSHANA, O ;
SCHILD, HO .
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1959, 14 (01) :48-58
[2]   EFFECT OF A CRUDE EXTRACT OF MANDEVILLA-VELUTINA ON CONTRACTIONS INDUCED BY BRADYKININ AND [DES-ARG9]-BRADYKININ IN ISOLATED VESSELS OF THE RABBIT [J].
CALIXTO, JB ;
YUNES, RA .
BRITISH JOURNAL OF PHARMACOLOGY, 1986, 88 (04) :937-941
[3]   BLOCKADE OF KININ-INDUCED RESPONSES OF THE GUINEA-PIG ISOLATED URINARY-BLADDER BY THE EXTRACT OF MANDEVILLA-VELUTINA [J].
CALIXTO, JB ;
YUNES, RA .
GENERAL PHARMACOLOGY, 1990, 21 (03) :285-290
[4]   THE SELECTIVE ANTAGONISM OF BRADYKININ ACTION ON RAT ISOLATED UTERUS BY CRUDE MANDEVILLA-VELUTINA EXTRACT [J].
CALIXTO, JB ;
NICOLAU, M ;
YUNES, RA .
BRITISH JOURNAL OF PHARMACOLOGY, 1985, 85 (04) :729-731
[5]   KININ ANTAGONIST ACTIVITY OF COMPOUNDS FROM MANDEVILLA-VELUTINA IN THE RAT ISOLATED UTERUS [J].
CALIXTO, JB ;
NICOLAU, M ;
PIZZOLATTI, MG ;
YUNES, RA .
BRITISH JOURNAL OF PHARMACOLOGY, 1987, 91 (01) :199-204
[6]   ANTAGONISTIC EFFECT OF MANDEVILLA-VELUTINA EXTRACT ON KININ-INDUCED CONTRACTIONS OF GUINEA-PIG AND CAT ILEUM LONGITUDINAL SMOOTH-MUSCLE [J].
CALIXTO, JB ;
NICOLAU, M ;
YUNES, RA .
GENERAL PHARMACOLOGY, 1988, 19 (04) :595-599
[7]  
CALIXTO JB, 1988, BRAZ J MED BIOL RES, V21, P1015
[8]   ANTAGONISM OF KININ-INDUCED CONTRACTION OF ISOLATED RAT UTERUS BY THE CRUDE HYDROALCOHOLIC EXTRACT FROM MANDEVILLA-ILLUSTRIS [J].
CALIXTO, JB ;
YUNES, RA .
GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM, 1991, 22 (01) :99-101
[9]   THE COMPETITIVE ANTAGONISTIC EFFECT OF COMPOUNDS FROM MANDEVILLA-VELUTINA ON KININ-INDUCED CONTRACTIONS OF RAT UTERUS AND GUINEA-PIG ILEUM INVITRO [J].
CALIXTO, JB ;
PIZZOLATTI, MG ;
YUNES, RA .
BRITISH JOURNAL OF PHARMACOLOGY, 1988, 94 (04) :1133-1142
[10]  
CALIXTO JB, 1991, BRADYKININ ANTAGONIS, P97