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体外测定青蒿琥酯钠(SA)对大鼠红细胞膜Na~(+)-K~(+)-交换ATP酶活性的影响.方法:在反应系统中分别加入不同浓度的SA(0,0.5,1,5和10 μmol·L~(-1)),通过测定反应系统中释放的无机磷含量,计算酶活性.结果:随着SA浓度(O,0.5,1,5和10 μmol·L~(-1))的增高,对Na~(+)-K~(+)-交换ATP酶活性的抑制作用也随之增强,抑制率分别为15％,29％,46％和75％.将底物ATP浓度增加为125,250,375和500 μmol·L~(-1),进行了酶的动力学测定.用直线回归分析作Eadie-Hofstee动力学曲线,结果表明,SA对该酶的抑制作用为竞争性抑制.结论:提示SA可影响宿主红细胞膜的离子转运及膜的功能.
The effect of artesunate sodium (SA) on the ATPase activity of Na ~ (+) - K ~ (+) - exchange in rat erythrocyte membrane was determined in vitro.Methods: SA was added to the reaction system at different concentrations , 1,5 and 10 μmol·L -1), and the enzyme activity was calculated by measuring the content of inorganic phosphorus released from the reaction system.Results: With the concentration of SA (O, 0.5, 1, 5 and 10 μmol·L ~ (-1)) increased the inhibitory effect on the activity of Na ~ (+) - K ~ (+) - exchange ATPase with the inhibitory rates of 15%, 29%, 46% and 75%, respectively. The ATP concentration of the substrate was increased to 125, 250, 375 and 500 μmol·L -1, and the enzyme kinetics was measured.The linear regression analysis of Eadie-Hofstee kinetics curve showed that the inhibitory effect of SA on the enzyme was Competitive inhibition.Conclusion: It is suggested that SA can affect the ion transport and membrane function of host erythrocyte membrane.