阔叶十大功劳中双苄基异喹啉生物碱对离体大鼠主动脉的作用。

Effect of bisbenzylisoquinoline alkaloids from Mahonia aquifolium on the isolated rat aorta.

Sotníková R, Kost'álová D, Vaverková S

Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava.

Gen Pharmacol. 1994 Nov;25(7):1405-10. doi: 10.1016/0306-3623(94)90165-1.

Abstract

The extract from roots of Mahonia aquifolium as well as berbamine and oxyacanthine relaxed K(+)-precontracted rat aortal rings with IC50 values of about 20 mumol/l. 2. Relaxation was not inhibited by denudation of the endothelium or by premedication of the aortas with indomethacin, methylene blue or propranolol. 3. Berbamine and oxyacanthine inhibited contractions induced by noradrenaline, phenylephrine and serotonin in a non-competitive manner. Further, they competitively blocked calcium-induced contraction in Ca(2+)-free depolarizing PSS. 4. The blockade of calcium entry appears to be the main mechanism of the dilatory effect of the drugs tested, but their interaction with alpha-adrenoceptors could not be excluded.

摘要

阔叶十大功劳根提取物以及小檗胺和刺檗碱可使K⁺预收缩的大鼠主动脉环舒张，IC50值约为20 μmol/L。2. 内皮剥脱或用吲哚美辛、亚甲蓝或普萘洛尔对主动脉进行预处理均不抑制舒张。3. 小檗胺和刺檗碱以非竞争性方式抑制去甲肾上腺素、苯肾上腺素和5-羟色胺诱导的收缩。此外，它们在无钙去极化的生理盐溶液中竞争性阻断钙诱导的收缩。4. 钙内流的阻断似乎是所测试药物舒张作用的主要机制，但不能排除它们与α-肾上腺素能受体的相互作用。