摘要
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。
To study the mechanism of HSA interacting with ephedrine hydrochloride （EH） and pseudoephedrine hydrochloride （PH） under room temperature （25 ℃ ） and the physiological t^mperature （37℃ ）, the secondary structure modification and the thermodynamics of HSA-EH and HSA-PH interactions were investigated by circular dichroism （CD） and isothermal titration calorimetry （ITC）. The CD result showed that the secondary structure of HSA changed when interacting with EH and PH independently, indicating that HSA binds with EH and PH, an obvious temperature depending on these interaction under 25℃ - 37℃ was not observed. A series of thermodynamics parameters including association constants （ Kb ）, stoichiometry （N）, entropy （△S） and enthalpy （△H） were obtained by ITC analysis. A better conformational freedom was observed on HSA-PH interaction. The coupling of CD and ITC analysis could be a good method for rapid drug analysis.
出处
《分析试验室》
CAS
CSCD
北大核心
2014年第4期432-435,共4页
Chinese Journal of Analysis Laboratory
基金
广西自然科学基金项目(2011GXNSFB018028)资助
