左氧氟沙星和氧氟沙星与清蛋白的结合位点及荧光淬灭分析  

Fluorescence Quenching and Binding Sites Analysis of Levofloxacin and Ofloxacin with Human Serum Albumin

作　　者：王志强[1] 张梅君[1] 吴继禹[1] 王学宝[2] 黄学荪[1] 张秀华[1] 

机构地区：[1]温州医学院附属第一医院药剂科,325000 [2]温州医学院药学院分析测试中心,325035

出　　处：《医药导报》2012年第3期298-301,共4页Herald of Medicine

摘　　要：目的研究左氧氟沙星和氧氟沙星与人血清清蛋白的结合作用。方法通过荧光光谱法分析左氧氟沙星和氧氟沙星对人血清清蛋白荧光淬灭光谱,同步荧光光谱,根据热力学方程讨论两者间主要的作用力类型。结果在生理条件(pH=7.43,7℃)下,根据Stem-Volmer方程和荧光淬灭双倒数图,左氧氟沙星和氧氟沙星对人血清清蛋白淬灭类型为静态淬灭,左氧氟沙星对人血清清蛋白的结合常数K=1.46×105 L.mol-1,结合位点n=1.11,氧氟沙星对人血清清蛋白的结合常数K=4.31×104 L.mol-1,结合位点n=1.04,根据热力学方法确定作用力类型均为疏水作用力。结论与左氧氟沙星比较,氧氟沙星对人血清清蛋白的荧光淬灭减弱,结合常数和结合位点均变小,结合位置也有明显区别;这些数据给研究左氧氟沙星和氧氟沙星的药理作用和生物学效应,以及左氧氟沙星和氧氟沙星对蛋白质构象的影响等提供了重要信息。Objective To investigate the binding interaction of levofloxacin and ofloxacin with human serum albumin（HSA）by fluorescence spectrophotometry.Methods The interaction of levofloxacin and ofloxacin with HSA was studied by measuring fluorescence quenching spectra,synchronous fluorescence spectra.The type of binding force was estimated according to thermodynamic equation.Results According to Stem-Volmer equation and double-reciprocal equation under physiological condition（pH=7.4,37 ℃）,the type of fluorescence quenching of levofloxacin was found to be static quenching,the binding constant was 1.46×105 L·mol-1 and the binding sites was 1.11;the type of fluorescence quenching of ofloxacin also was static quenching,the binding constant was 4.31×104 L·mol-1 and binding sites was 1.04.The interaction between Levofloxacin and HSA was mainly driven by hydrophobic force which was the same as Ofloxacin.Conclusion The fluorescence quenching,combining constants and binding sites of ofloxacin with HAS were less than those of levofloxacin,which provides important information for studing the pharmacological effects,biological characteristics and configuration modification of levofloxacin and ofloxcin with HSA.

关 键 词：左氧氟沙星 氧氟沙星 清蛋白 荧光淬灭 

分 类 号：R978.19[医药卫生—药品] R969.3[医药卫生—药学]