荧光法研究盐酸拓扑替康、盐酸依利替康喜树碱类药物和牛血清白蛋白的相互作用  

Study on the Interaction between Bovine Serum Albumins and Topotecan Hydrochloride or Irinotecan Hydrochloride

作　　者：李桂芝[1] 刘永明[1] 虢新运[1] 王进军[1] 

机构地区：[1]烟台大学化学学院,烟台264005

出　　处：《化学学报》2006年第7期679-685,共7页Acta Chimica Sinica

基　　金：国家科技部中韩政府间合作(2002)资助项目.

摘　　要：用荧光光谱法、分光光度法研究了盐酸拓扑替康(Topotecanhydrochloride,简记为THC)与盐酸依利替康(Irinotecanhydrochloride,简记为IHC)两种喜树碱类药物与牛血清白蛋白(Bovineserumalbumins,BSA)的相互结合反应.实验表明喜树碱类药物与牛血清白蛋白的相互结合作用为单一的静态猝灭过程,在溶液中二者以物质的量比1∶1牢固结合,25℃时其结合反应的平衡常数K0分别为:K0,THC=7.73×105L?mol-1,K0,IHC=4.73×105L?mol-1.根据F?rster非辐射能量转移机理,求算了给体(BSA)与受体(喜树碱类药物)间距离r和能量转移效率E分别为:rTHC=3.75nm,rIHC=3.08nm,ETHC=0.26,EIHC=0.51.并研究了五种离子对喜树碱类药物与BSA结合作用的影响,推测了二者之间的主要作用力为疏水作用和偶极-偶极相互作用.The binding reaction between camptothecin derivatives, such as topotecan hydrochloride （THC） and irinotecan hydrochloride （IHC）, and bovine serum albumins （BSA） was studied by fluorescence and UV-Vis absorption spectra. The research results indicate that the combination reaction of them was a single static quenching process, and camptothecin derivatives strongly bound BSA with the molar ratio of 1 ： 1 and the binding equilibrium constant K0 at 25 ℃, K0.THC=7.73×10^5 L/mol, K0,IHC=4.73×10^5 L/mol. The shortest binding distance r and energy transfer efficiencies E between donor BSA and acceptor of camptothecin derivatives were obtained by Forster nonradiative energy transfer mechanism as follows, r^THC=3.75 nm, r^IHC=3.08 nm and E^THC=0.26, E^IHC=0.51. And the effect of some ions on the binding reaction between camptothecin derivatives and BSA was investigated to find the main sort of binding force between them to be both hydrophobic force and dipole force.

关 键 词：盐酸拓扑替康 盐酸依利替康 喜树碱类药物 牛血清白蛋白 荧光猝灭 结合反应 

分 类 号：R96[医药卫生—药理学]