牛血清白蛋白与头孢菌素相互作用的荧光法研究

研究血清白蛋白与药物分子之间的作用,对于理解具有生物活性的物质与蛋白质之间的相互作用机理很重要;有助于从分子水平上理解药物在体内的运输和代谢过程;对于阐明药物的作用机制、药代动力学以及蛋白质构象变化都有重要意义.本文通过荧光光谱和紫外-可见吸收光谱,研究了牛血清白蛋白与头孢菌素一代、二代和三代代表药物的作用机理,包括头孢拉定、头孢呋辛和头孢噻肟.详细讨论了牛血清白蛋白与头孢菌素作用的各种参数,包括猝灭参数、结合参数、热力学参数和作用模式等.推测头孢菌素是通过与牛血清白蛋白分子结构中Trp 212附近的活性位点相结合而导致荧光猝灭的.

Study on the Interaction between Bovine Serum Albumin and Cephalosporin by Fluorescence Spectroscopy

The binding mechanism of bovine serum albumin(BSA) with cephalosporin analogues including cefradine,cefuroxime and cefotaxime was investigated adopting fluorescence and absorption spectra.It was shown that the intrinsic fluorescence of BSA was quenched by the drugs through the static quenching and nonradiative engergy transferring procedure.The binding parameters including the association constant and the number of binding potential point were calculated at different temperatures,and thermodynamic parameters ΔH°,ΔS° and ΔG° were given.The binding mode of BSA with cephalosporin showed that the hydrophobic interaction might play a major role.