盐酸安非他酮与牛血清白蛋白相互作用的NMR研究  

Nuclear Magnetic Resonance Study on Interaction between Bupropion and Bovine Serum Albumin

作　　者：许慧芳[1] 叶锦珠[1] 吴霞晖[1] 林庚蓉 张美玲[2] 

机构地区：[1]广东省珠海市妇幼保健院,广东珠海519000 [2]温州医科大学药学院,浙江温州325035

出　　处：《分析测试学报》2014年第1期45-50,共6页Journal of Instrumental Analysis

基　　金：国家自然科学基金项目(81102310)

摘　　要：利用核磁共振波谱(NMR)技术研究盐酸安非他酮与牛血清白蛋白(BSA)的相互作用,分析盐酸安非他酮溶液在加入BSA前后化学位移、纵向弛豫时间(1H T1)、二维核Overhauser效应谱(2D NOESY)等的变化信息。结果显示,BSA的加入可使盐酸安非他酮的H原子化学位移向高场移动、1H T1值缩短、NOE交叉峰增多;利用不同浓度盐酸安非他酮在0.2 mmol/L BSA蛋白溶液中的自扩散系数拟合得到两者的结合常数为0.34 mmol/L,结合位点数为11。盐酸安非他酮与牛血清白蛋白的结合是多位点的弱结合。该研究对于临床安全、合理使用盐酸安非他酮及设计改良类似药物具有重要意义。The interaction between bupropion hydrochloride and bovine serum albumin （BSA） was studied based on 1 H nuclear magnetic resonance （1H NMR） chemical shift,Longitudinal relaxation time（1H T1）,2D nuclear overhauser spectroscopy（2D NOESY） and diffusion coefficient.The results showed that the presence of BSA could resulted in the significantly decrease in the chemical shifts of bupropion protons as well as the spin-lattice relaxation time,and the increase in the NOE cross peak.The apparent dissociation constant was 0.34 mmol/L and the binding sites of bupropion molecules on BSA was 11.Therefore,the reaction of bupropion and BSA was a combination of a number of weak points.The present study is of great importance for the safe and rational use of bupropion in clinic,and the development of improved bupropion analogs.

关 键 词：核磁共振 盐酸安非他酮 弛豫时间 2D NOESY 自扩散系数 

分 类 号：O657.3[理学—分析化学] O629.73[理学—化学]