光谱法研究甲啶铂与牛血清白蛋白的相互作用  

Spectroscopic study of the interaction between picoplatin and bovine serum alb umin

作　　者：丁浩 叶满萍 彭娟 胡劲[2] 普绍平 丛艳伟 王应飞 DING Hao;YE Man-ping;PENG Juan;HU Jing;PU Shao-ping;CONG Yan-wei;WANG Ying-fei(College of Optical and Electronic Technology,China Jiliang University,Hangzhou 310018,China;Faculty of Materials Science and Engineering,Kunming University of Science and Technology,Kunming 650093,China;Guiyan Pharmaceutical Co.Ltd.,Kunming 650106,China)

机构地区：[1]中国计量大学光学与电子科技学院,浙江杭州310018 [2]昆明理工大学材料科学与工程学院,云南昆明650093 [3]昆明贵研药业有限公司,云南昆明650106

出　　处：《光电子．激光》2021年第1期70-77,共8页Journal of Optoelectronics·Laser

基　　金：国家自然科学基金(21103155);云南省科技计划项目(2016DH008)资助项目。

摘　　要：甲啶铂(picoplatin)是一种新型的抗癌药物,但其在体内的作用机制尚不明确。利用荧光光谱技术研究模拟人生理条件(Tris-HCl缓冲溶液体系,pH7.4)下甲啶铂与牛血清白蛋白(BSA)的相互作用,甲啶铂对BSA的内源荧光(336nm)有猝灭作用。在室温296K和模拟人体温度310K条件下,甲啶铂对BSA的荧光猝灭效率随温度升高而降低,属于静态猝灭。运用位点模型计算出296K、310K时结合常数分别为4.032×10^(4)、2.181×10^(5)L·mol^(-1),结合位点数分别为1.10、1.31,说明甲啶铂对BSA的靶向目标仅有一个。根据计算所得的热力学参数ΔH>0,ΔS>0,说明甲啶铂与BSA分子之间以疏水作用力为主,且结合反应为吸 热反应。时间分辨荧光结果表明,BSA中第212位Trp残基可能是甲啶铂的靶向目标,且温度升高有利于甲啶铂与BSA反应的正向进行。Picoplatin is a kind of new cancer drugs,but its mechanism of action in the body is not clear.Using fluorescence spectroscopy technology to study the interaction between picoplatin and bovine serum albumin (BSA) under simulated human physiological conditions(Tris-HCL buffer solution system,pH7.4),picoplatin has a quenching effect on the endogenous fluorescence (336nm) of BSA.Under the condition of room temperature 296K and simulated human temperature of 310K,the fluorescence extinction efficiency of picoplatin to BSA decreases with the increase of temperature,which belongs to static annihilation.The binding constants at 296K and 310K were 4.032×10^(4) and 2.181×10^(5)L·mol^(-1),respectively,and the number of binding sites were 1.0955and 1.3105,respectively,indicating that picoplatin had only one target for BSA.According to the calculated therm odynamic parameters of ΔH>0and ΔS>0,it is shown that the hydrophobic force is mainly between the picoplatin and the BSA molecule,and the combined reaction is a heat-absorbing reaction.The results of time-resolution fluorescence sh ow that the 212th Trp residue in the BSA may be the target of picoplatin,and the increase of temperature is favorable for the forward reaction of picoplatin with BSA.

关 键 词：甲啶铂 牛血清白蛋白 荧光光谱 热力学参数方程 时间分辨荧光光谱 

分 类 号：O657.3[理学—分析化学]