光谱法研究头孢地尼与牛血清白蛋白的相互作用

发布时间：2018-10-13 09:06

【摘要】：目的:研究头孢地尼(cefdinir,CE)与牛血清白蛋白(bovine serum albumin,BSA)之间的相互作用。方法:在优化的实验条件下,运用荧光光谱和紫外-可见光谱法研究CE与BSA之间的相互作用。结果:CE可与BSA形成基态复合物,从而猝灭BSA的内源性荧光,猝灭机制为静态猝灭。通过计算获得了二者在不同温度下的结合常数及结合位点数。通过计算反应热力学参数值,可推断CE与BSA作用力主要为氢键和范德华力,生成的自由能变(Gibbs free energy change,ΔG)为负值,表明CE与BSA的作用过程是一个自发过程。两者的结合部位主要位于亚螺旋域II A中。Hill系数小于1,表明CE有负协同作用。同步荧光光谱表明CE对BSA构象不产生影响,结合位点更接近于酪氨酸。结论:该实验对揭示药物动力学问题及后续头孢类药物的研究开发提供了理论依据。
[Abstract]:Objective: to study the interaction between cefdinir (cefdinir,CE) and bovine serum albumin (bovine serum albumin,BSA). Methods: the interaction between CE and BSA was studied by fluorescence spectra and UV-Vis spectra under optimized experimental conditions. Results: CE can form a ground state complex with BSA, thus quenching the endogenous fluorescence of BSA. The quenching mechanism is static quenching. The binding constants and binding sites of the two are calculated at different temperatures. By calculating the thermodynamic parameters of the reaction, it can be inferred that the interaction between CE and BSA is mainly hydrogen bond and van der Waals force, and the generated free energy changes (Gibbs free energy change, 螖 G to negative value, which indicates that the interaction between CE and BSA is a spontaneous process. The binding sites were mainly located in the subhelical domain II A, and the Hill coefficient was less than 1, which indicated that CE had negative synergistic effect. Synchronous fluorescence spectra showed that CE had no effect on the conformation of BSA and the binding site was closer to tyrosine. Conclusion: this experiment provides a theoretical basis for revealing the pharmacokinetic problems and the further research and development of cephalosporins.
【作者单位】：曲靖师范学院化学化工学院;
【基金】：国家自然科学基金(21261019) 云南省教育厅科学研究基金(2015C090Y)~~
【分类号】：R96;O657.3

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