2-(4-甲基苯基)-3-(N-乙酰基)-5-(2-羟基苯基)-1,3,4-噁唑啉的合成及与人血清白蛋白的相互作用

摘要

合成了2-(4-甲基苯基)-3-(N-乙酰基)-5-(2-羟基苯基)-1,3,4-噁唑啉(MPAHO),并用核磁共振波谱法和红外光谱法对其进行了表征.采用荧光光谱技术研究了MPAHO与人血清白蛋白(HSA)的相互作用.结果表明:MPAHO对HSA有较强的荧光猝灭作用,根据Stern-Volmer方程得到的荧光猝灭常数,可判断由于与MPAHO反应而导致HSA的荧光猝灭均属于静态猝灭.采用位点结合模型公式和F(o)rster非辐射能量转移理论计算了结合常数、结合位点数、结合距离.从计算得到的热力学参数焓变△H和熵变△S,推断MPAHO与HSA之间的作用力为静电引力.并应用同步荧光光谱和三维荧光技术研究了MPAHO对HSA构象的影响.%2-(4-Methylphenyl)-3-(N acetyl) 5-(2-hydroxyphenyl)-1,3,4-oxodiazoline (MPAHO) was synthesized and characterized by NMR and IR.The mechanism of the interaction between MPAHO and human serum albumin (HSA) was studied by fluorospectrometry.Significant quenching of fluorescence of HSA was observed by its reaction with MPAHO.Judging from the fluorescence quenching constants obtained by SternVolmer equation,fluorescence quenching of HSA by MPAHO was attributed to static quenching.The binding constants,number of binding sites and binding distance were found by applying the equation of site-binding model and F(o)rster nonradiative energy transfer theory.Values of thermodynamic parameters △H and △S were calculated and based on these results,the binding force between MPAHO and HSA was recognized to be electrostatic attraction.The effect of MPAHO on the conformation of HSA was studied by synchronous fluorospectrometry and three-dimensional fluorescence technology.