5种抗血小板药对大鼠肝酪蛋白激酶Ⅱ的影响

Effects of five antiplatelet agents on casein kinase Ⅱ from rat liver

用ＤＥＡＥ－纤维素和肝素－Ｓｅｐｈａｒｏｓｅ４Ｂ层析法部分纯化了大鼠肝酪蛋白激酶Ⅱ（ＣＫⅡ）；研究了５种抗血小板药对ＣＫⅡ活性的影响。结果表明，肝素对ＣＫⅡ有强烈的抑制作用，其ＩＣ５０为０．８８ｍｍ·Ｌ－１；蝙蝠葛碱、川芎嗪对ＣＫⅡ有明显的抑制作用（Ｐ＜０．０１），但较肝素的作用弱得多；汉防己碱对ＣＫⅡ活性没有明显影响；而潘生丁能使ＣＫⅡ活性明显升高，在一定范围内呈剂量依赖关系。这些结果可能对研究ＣＫⅡ是否在血小板的聚集和活化中起某些作用有重要的参考价值。

Abstract Casein kinase Ⅱ(CKⅡ) was partially purified from rat livers by sequential DE52 and heparin-Sepharose 4B chromatography,and characterized;effects of five antiplatelet agents on the enzyme were investigated.We found that heparin strongly inhibited the activity of CK ⅡWith IC50 0.88 mg·L-1;dauricine(Dan)、ligustrasine(Lig)had significant inhibitory effects on CK Ⅱ,but their effects were much more weaker than heparin's,tetrandricine(Tet) had no effect on the activity of CK Ⅱ ;but dipyridamole(Dip)displayed significantly active effect on CK Ⅱ with dose-dependent response in a range of concentrations between 62.5 μmol· L-1 and 500μmol· L-1.These results may have important implication in studying if CKⅡ play some roles in platelet activation and aggregation.