小檗碱与牛血清白蛋白相互作用的核磁共振研究  

Nuclear Magnetic Resonance Studies on Interactions of Berberine and Bovine Serum Albumin

作　　者：吴丽敏[1] 张美玲[1] 娄依依[1] 李旸[1] 赵良才 黄可新[1] 高红昌[1] 

机构地区：[1]温州医学院药学院,温州325035 [2]中科院上海药物研究所新药研究国家重点实验室,上海201203

出　　处：《分析化学》2011年第8期1223-1227,共5页Chinese Journal of Analytical Chemistry

基　　金：国家自然科学基金(No.20705037);浙江省医药卫生专项(No.2010QNA016)资助

摘　　要：采用核磁共振波谱技术(NMR)研究小檗碱与牛血清白蛋白(BSA)的相互结合作用。比较不同浓度小檗碱在一定浓度的BSA溶液中的化学位移、弛豫时间和扩散系数的变化情况。研究表明,小檗碱环上芳香质子与BSA的结合作用较强,其它烷基质子与BSA结合作用较弱;BSA的结合使得小檗碱各个质子的1 HT1弛豫时间明显减少,质子在溶液中运动受限;小檗碱与BSA相互作用的饱和浓度之比为60∶1;根据自扩散系数拟合可以得到两者解离常数为0.44mmol/L;结合位点数为22。本研究为临床安全、合理使用小檗碱,以及开发改良小檗碱类似药物提供实验依据。1H nuclear magnetic resonance chemical shift,relaxation time and diffusion coefficient measurements were carried out to study the interaction on the affinity binding of Berberine,an antibacterial drug,to bovine serum albumin（BSA）.The results showed that the protons of aromatic ring of Berberine were more favorable to form Berberine-BSA complex than those of aliphatic groups.BSA combination resulted in significantly decrease in the relaxation time of Berberine protons,which suggests that the motion of these protons were limited in aqueous solutions.The saturation concentration ratio of Berberine to BSA is 60 ∶ 1 according to the measurements of chemical shift and relaxation time.The apparent dissociation constant was 0.44 mmol/L and the binding sites of Berberine molecules on BSA was 22 fitted from the self-diffusion measurements.This study is of great importance for the safe and rational use of Berberine in clinic,and development of improved Berberine analogs.

关 键 词：核磁共振 小檗碱 牛血清白蛋白 弛豫时间 自扩散系数 

分 类 号：R284[医药卫生—中药学] Q6-33[医药卫生—中医学]