一种蛋白-药物结合常数的测定方法

目的建立一种蛋白-药物结合常数的测定新方法。方法以固定化牛血清白蛋白为固定相,磷酸盐缓冲溶液为流动相,获得不同进样量下药物的液相色谱保留参数,以溶质进样量与保留值的关系方程进行拟合,计算蛋白-药物结合常数(直接进样法)。结果测定了咖啡酸(CA),汉黄芩素(WO)和木犀草素(LU)3种药物与固定化牛血清白蛋白(BSA)在人体生理条件(37℃,pH7.40)下的结合常数,其数值高于竞争置换法,但与相关文献数据接近。结论直接进样法可作为一种新方法用于研究蛋白-药物的相互作用。

A method to determine association constants of protein-drug interaction

Aim A new method was established to determine the association constants of protein-drug interaction.Methods Using immobilized bovine serum albumin(BSA) as stationary phase,phosphate buffer as mobile phase,retention parameters of drugs in liquid chromatography were obtained in different injected amounts,and retention factors were fitted by the equation describing the relationship between the injected amount of solutes and retention factors to calculate the association constants of protein-drug interaction(direct injected methods).Results The present method was used to determine the association constants of three kinds of drugs,caffeic acid(CA),wogonin(WO) and luteolin(LU),with immobilized bovine serum albumin(BSA) under human physiological condition(37℃,pH 7.40),and the obtained association constants were higher than those from zonal elution,but close to the data from the related literatures.Conclusion Direct injected method can be used as a new method to investigate protein-drug interaction.