白藜芦醇类似物与人血清白蛋白的相互作用

摘要

采用荧光光谱、三维荧光光谱、紫外吸收光谱研究白藜芦醇类似物(Z)-2-(3,4-二甲氧苯基)-3-(4-二甲氨基苯基)丙烯腈(HCQ)与人血清白蛋白(HSA)的相互作用,探讨其作为抗肿瘤药物的可能.结果发现HCQ与HSA形成了基态配合物,HCQ主要结合于HSA的位点Ⅰ,与位点Ⅱ也有微量的结合,反应为自发的放热反应,其△H、△S、△G均小于零,二者之间的结合力为氢键或者范德华力,结合常数为104～105数量级.HCQ与HSA的结合使HSA构象发生变化,Trp-214所处的环境疏水性增加,使得其内源性荧光显著降低.说明合成的白藜芦醇类似物能够与人血清白蛋白结合.%To study the features of interaction between resveratrol analogues (Z)-2-( 3,4-dimethoxy phenyl)-3-(4-dimethylaminophenyl) acrylonitrile( HCQ)and human serum albumin(HAS) ,and explore the possibility of HCQ as an anticancer drugs,the binding of the stilbene compound to human serum albumin (HAS) was studied using fluorescence spectroscopy, three-dimensional fluorescence spectrum ,and UV-Vis absorption spectroscopy. The results showed that the interaction of HCQ and HAS lead to the formation of a new compound in ground state,the primary binding site was site I ,a trace bind with site IS at the same time. The reaction was spontaneous and exothermic,the thermodynamic parameters( △H.,△S,△G) was less than zero,the binding force was hydrogen bond or van der waals force,the binding constant was calculated to be in the order of 104 - 10s. The binding changed the conformation of HAS and enhanced the hydrophobicity of the environment of the Trp-214 residue,resulted in the significantly decreasing of the fluorescence of HAS These results illustrated that HCQ can bind with HAS and so can be transported in viva