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。
Objective:To explore the interaction between cefdinir(CE) and bovine serum albumin(BSA) by fluorescence and ultraviolet-visible absorption spectrometry.Methods:Under the optimal conditions,the interaction between CE and BSA was investigated by fluorescence and ultraviolet-visible absorption spectrometry.Results:CE could quench(static quenching) the intrinsic fluorescence of BSA by forming the CE-BSA complex.The main binding forces were considered as hydrogen bonds and Van der Waals forces based on the calculated values of the thermodynamic parameter.The process of binding was spontaneous because Gibbs free energy change was negative.The primary binding site for CE was located at sub-domain Ⅱ of BSA.The values of Hill’s coefficients were less than 1,indicating a negative cooperative effect.Synchronous fluorescence spectra showed that the conjugation reaction between CE and BSA did not affect the conformation of BSA,and the binding site was close to the tyrosine residue.Conclusion:This test provides a theoretical basis for revealing the pharmacokinetic issue and the development for new drugs.
出处
《中南大学学报（医学版）》
CAS
CSCD
北大核心
2015年第9期979-986,共8页
Journal of Central South University ：Medical Science
基金
国家自然科学基金(21261019)
云南省教育厅科学研究基金(2015C090Y)~~
关键词
头孢地尼
荧光猝灭
相互作用
cefdinir
fluorescence quenching
interaction
