小檗碱衍生物CPU-86017与小檗碱的抑制血管收缩活性的比较(英文)  

Comparison of Inhibitory Activity of Berberine Derivative CPU 86017 and Berberine on Vascular Contractions

作　　者：戴德哉[1] 何毅[1] 黄凤华 朱益 汗护森[1] 

机构地区：[1]中国药科大学药理学研究室,南京210009

出　　处：《中国药科大学学报》2000年第6期447-450,共4页Journal of China Pharmaceutical University

摘　　要：本文通过抑制离体血管平滑肌的收缩， 比较CPU-86017与小檗碱对抗胞内钙动员与外钙内流的活性。观察对3类血管收缩的抑制强度，以苄普地尔为阳性对照。（1）大鼠主动脉环在含钙K-H液中加100 mmol·L-1 KCl的收缩；（2）大鼠主动脉环在无钙K-H液中KCl 100 mmol·L-1的收缩；（3）在无钙K-H液中再加2.5 mmol·L-1CaCl2的收缩。 CPU-86017 30，100，300 μmol·L-1 剂量依赖性地抑制含钙K-H液中高钾引起的收缩，而小檗碱较弱。在无钙K-H液中、CPU-86017在低浓度时抑制血管收缩作用强于小檗碱。 在无钙K-H液中加入钙离子后，CPU-86017剂量依赖性地抑制血管收缩，而小檗碱直到300 μmol·L-1才显示抑制作用。小檗碱中度抑制由胞内钙动员和外钙内流的血管收缩。与之相比，CPU-86017明显增强抑制外钙内流。To compare the effect of CPU 86017 and berberine o n intracellular calcium mobilization and calcium entry by suppression on isolate d vascular smooth muscle (VSM)contraction. CPU-86917, berberine and bepridil we re applied to suppress three kinds of vascular contractions: (1)In the K-H sol ution, rat aortic rings were contracted (phase I contraction) after adding 100 mm ol·L{-1} KCl, (2)In Ca{2+}-free K-H solution, and (3) by adding 2.5 mmol·L{-1} CaCl-2. In K-H solution with normal Ca{2+}, contractions induced by high K+ can be suppressed by CPU-86017 at 30, 100, 300 mmol· L -1 in a dose-dependent manner, while berberine was less effective. In Ca {2+}-free K-H solution, CPU-86017 was more potent to suppress VSM contr action at low concentrations than berberine. After adding Ca2+ into the Ca{2+}-free K-H solution, CPU-86017 suppressed VSM contractions in a do se-dependent manner; whereas berberine exerted no significant inhibition until 300mol·L-1. Berberine showed a moderate inhibition on VSM contraction by suppressing intracellular release of calcium and calcium entry. CPU-86017 is potentiated with its suppression mainly on calcium entry compared with its sta rting material berberine.

关 键 词：钙 血管平滑肌 小檗碱 CPU-86017 苄普地尔 

分 类 号：R965[医药卫生—药理学]