摘要
在模拟人体生理条件下,用紫外-可见吸收光谱法和荧光光谱法研究盐酸利多卡因(LH)和牛血清白蛋白(BSA)的相互作用及Mg^(2+)、Fe^(3+)、Cu^(2+)、Co^(2+)和Cr^(3+)对两者的结合作用的影响.结果表明:LH对BSA的荧光有猝灭作用,其猝灭过程属于动态猝灭.根据热力学参数确定了LH和BSA之间的作用力类型主要为氢键和范德华力.LH可以被BSA运输且结合位点位于BSA的亚螺旋域ⅢA中.Hill系数略大于1,表明LH对BSA的结合为较弱的正协同作用.LH对BSA构象产生微弱影响,结合位点更接近于酪氨酸.金属离子对结合产生促进作用,延长药物作用时间并减弱药物毒性.对揭示药物动力学问题及后续麻醉类药物的研发提供了理论依据.
Under the condition of simulation of human body physiology, the interaction of lidocaine hydrochloride （LH） with bovine serum albumin （BSA） and the effect of Mg2＋, Fe3＋, Cu2＋, Co2＋ and Cr2＋ on the binding of LH with BSA were studied with UV-visible absorption spectra and fluorescence spectra. The result showed that the fluorescence of BSA would be quenched by LH, which was a dynamic quenching process. The category of interaction force between LH and BSA determined with thermodynam- ic parameters was mainly the hydrogen bond force and Vander Waals force. LH could be transported by BSA and the binding site was located at sub-helical domain Ⅲ A of BSA. The value of Hill coefficient would be slightly more than 1, indicating that the bonding of LH with BSA was a weaker positive coopera- tive effect. The LH would have a little effect on the conformation of BSA and the binding site was even closer to the tyrosine residue. The metal ions would promote on their bonding, prolong drug effect time, and reduce drug toxic, providing a theoretical basis for revealing the pharmacokinetic issue and further re- searching and developing of narcotic drugs.
出处
《兰州理工大学学报》
CAS
北大核心
2016年第5期73-76,共4页
Journal of Lanzhou University of Technology
基金
国家自然科学基金(21261019)
云南省教育厅科学研究基金(2015C090Y)
