黄连素片对钙离子通道的拮抗作用

Huangliansu Pian and its Calcium Channel Antagonistic Activity

本研究以药理学的方法检测了黄连素片对Ｃａ２＋通道的拮抗作用。结果表明黄连素片的水溶液能明显抑制Ｃａ２＋的内流．拮抗Ｌ型钙通道促进剂Ｂａｙｋ８６４４对钙通道的激活，从而降低ＳＤ大鼠胸主动脉的收缩性，４０μｇ／ｍｌ浓度的黄连素片对Ｃａ２＋通道的抑制作用与１０－８ｍｏｌ／Ｌ浓度的尼群地平相似。同时用Ｂａｙｋ８６４４使ＳＤ大鼠胸主动脉收缩后，黄连素片能以剂量依赖方式引发收缩动脉的自发性舒张。８０ｍｇ／Ｌ浓度的黄连素片能使１０－７ｍｏｌ／ＬＢａｙｋ８６４４所致的收缩血管基本达到１００％的舒张，其作用与１０－７ｍｏｌ／Ｌ的尼群地平相似。说明黄连素片具有抑制电压控制的钙通道的作用，这可能是它具有心血管药理作用的基础。

Huangliansu Plan, a crude extract of Rhizomata of Coptis, was studied for its calcium channel antagonistic activity.The result indicated that the aqua of Huangliansu Pian was able to reduce the contractile responses of aortic rings of Sprague-Dawley rats to Ca2+ through inhibiting Ca2+ influx and antagonizing Bay K 8644, a L-type calcium channel agonist, of which the activity of 40μg/ml Huangliansu Pian was similar to 10-8mol/L Nifedipine.Simultaneously, Huangliansu Plan was able to evoke the spontaneous relaxation of aortic rings in contraction tone induced by Bay K 8644, of which 80μg/ml Huangliansu Pian made them relax almost to 100%, with similar activity to 10-7 mmol/L Nifedipine. The results support the concept that voltage-operated calcium channel antagonism of Huangliansu Pian can contribute to its pharmacological effect on cardiological diseases.