VASODILATOR EFFECTS OF LIRIODENINE AND NORUSHINSUNINE, 2 APORPHINE ALKALOIDS ISOLATED FROM ANNONA-CHERIMOLIA, IN RAT AORTA

被引:9
作者
CHULIA, S [1 ]
NOGUERA, MA [1 ]
IVORRA, MD [1 ]
CORTES, D [1 ]
DOCON, MP [1 ]
机构
[1] UNIV VALENCIA, FAC FARM, DEPT FARMACOL, E-46100 BURJASSOT, SPAIN
关键词
ANNONA CHERIMOLIA; ANNONACEAE; LIRIODENINE; NORUSHINSUNINE; ALPHA-ADRENOCEPTOR AND CALCIUM CHANNEL;
D O I
10.1159/000139307
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effect of two aporphines, liriodenine and norushinsunine, isolated from Annona cherimolia, were studied in the rat aorta in order to examine their mechanism of action. Both alkaloids (10(-7)-10(-4) mol/l) showed relaxant effects on the contractions elicited by 10(-6) mol/l noradrenaline (NA) or 80 mmol/l KCl, but, while liriodenine showed a nonspecific relaxant action on both spasmogens, norushinsunine was more potent on KCl-induced contraction. In Ca2+-free medium, both alkaloids (0.1 mmol/l) inhibited the responses elicited by NA, but not those elicited by caffeine. This inhibitory action occurred when the alkaloids were present during the release of the Ca2+ internal stores or during the refilling process. These results suggest that the two aporphines show a relaxant action in rat aorta which is mediated by an interaction with alpha(1)-adrenoceptors and an alteration of the Ca2+ entry via voltage-operated channels. Norushinsunine exhibits a certain degree of selectivity as an L-type Ca2+ channel blocker.
引用
收藏
页码:380 / 387
页数:8
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