白藜芦醇类似物与人血清白蛋白的相互作用

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ΔH、ΔS、ΔG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。

Interaction between resveratrol analogue and human serum albumin

To study the features of interaction between resveratrol analogues(Z)-2-(3,4-dimethoxy phenyl)-3-(4-dimethylaminophenyl)acrylonitrile(HCQ)and human serum albumin(HSA),and explore the possibility of HCQ as an anticancer drugs,the binding of the stilbene compound to human serum albumin(HSA)was studied using fluorescence spectroscopy,three-dimensional fluorescence spectrum,and UV-Vis absorption spectroscopy.The results showed that the interaction of HCQ and HSA lead to the formation of a new compound in ground state,the primary binding site was site Ⅰ,a trace bind with site Ⅲ at the same time.The reaction was spontaneous and exothermic,the thermodynamic parameters(ΔH、ΔS、ΔG)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 104～105.The binding changed the conformation of HSA and enhanced the hydrophobicity of the environment of the Trp-214 residue,resulted in the significantly decreasing of the fluorescence of HSA.These results illustrated that HCQ can bind with HSA and so can be transported in vivo.