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在模拟储存温度(25℃)和生理温度(37℃)条件下,利用圆二色和等温滴定微量热技术获得了人血清白蛋白与盐酸麻黄碱、盐酸伪麻黄碱相互作用的热力学参数,探索了蛋白质二级结构的变化及其作用机制。圆二色光谱实验检测到人血清白蛋白与盐酸麻黄碱、盐酸伪麻黄碱相互作用后的二级结构发生变化,这种构象变化在25℃~37℃区间内的温度依赖性不明显。ITC检测获得一系列有关分子相互作用的热力学信息,包括结合常数(Kb)、反应的化学计量数(N)、熵(ΔS)和焓(ΔH)。发现人血清白蛋白在与盐酸伪麻黄碱结合时,表现出比盐酸麻黄碱更好的活跃度。圆二色和等温滴定微量热技术的联用为建立一套快速药物分析方法提供了可行性基础。
The thermodynamic parameters of interaction between human serum albumin and ephedrine hydrochloride and pseudoephedrine hydrochloride were obtained by using circular dichroism and isothermal titration calorimetry at simulated storage temperature (25 ℃) and physiological temperature (37 ℃) Secondary structure changes and its mechanism of action. Circular dichroism spectroscopy experiments detected the interaction of human serum albumin and ephedrine hydrochloride, pseudoephedrine hydrochloride secondary structure changes, this conformational change in the temperature range of 25 ℃ ~ 37 ℃ is not obvious. The ITC assay obtains a series of thermodynamic information about molecular interactions including the binding constant (Kb), the stoichiometry (N) of the reaction, entropy (ΔS) and enthalpy (ΔH). Human serum albumin was found to show better activity than ephedrine hydrochloride when combined with pseudoephedrine hydrochloride. The combination of circular dichroism and isothermal titration calorimetry provides a viable basis for establishing a rapid drug analysis method.