4-芳基-1,4-二氢吡啶衍生物的合成及与血清白蛋白的相互作用

摘要

4-Aryl-1,4-dihydropyridine derivatives were synthesized and characterized by FTIR,MS and 1H NMR. The interaction of the drug molecule(a)with bovine serum albumin(BSA)was studied by fluorescence. The Dynamic quenching constant Kq,the bind-ing constants Ka,the number of binding sites n and the thermodynamic parameters△H,△S of the drug molecule(a)with BSA were 5. 474×1011L·mol-1·s-1,1. 597 6×102L·mol-1,0. 642 2,-14. 58kJ·mol-1,-30. 27J·mol-1·K-1(△H＜0,△S＜0)at 300K. The results showed that drug molecule could cause fluorescence quenching of BSA,and the quenching mechanism was static quenching. The interaction force of the drug molecule and BSA was attributed to hydrogen bond and Van der Waals force.%合成并用红外光谱、质谱和核磁共振表征了4-芳基-1,4-二氢吡啶衍生物,利用荧光光谱法研究了药物分子a与牛血清白蛋白(BSA)分子间的相互作用.在300K时药物分子a与BSA之间相互作用的动态猝灭常数、结合常数和结合位点数分别为:K q＝5. 474×1011L·mol-1·s-1,Ka＝1. 597 6×102L·mol-1和n＝0. 642 2;热力学参数△H＝-14. 58 kJ·mol-1,△S＝-30. 27 J·mol-1·K-1(△H＜0,△S＜0).实验表明:药物分子可以使BSA发生荧光猝灭,其猝灭机理是形成基态复合物的静态猝灭;药物分子a与BSA的作用力为氢键和范德华力.