3-苯基-2-(4-叔丁基苯氧基)-3′-氧环己烷并噻吩并[2,3-d]嘧啶-4(3H)-酮的合成及其与BSA的相互作用

Synthesis of 3-Phenyl-2-(4-tert-butylphenoxy)-pentamethyleneoxide [3′,4-5,4]thienopyrimidin-4(3H)-one(PTP) and Interaction between PTP and Bovine Serum Albumin

通过Aza-Wittig反应,碳二亚胺与酚类化合物在碱性催化条件下成环,合成了3-苯基-2-(4-叔丁基苯氧基)-3′-氧环己烷并噻吩并[2,3-d]嘧啶-4(3 H)-酮(PTP)。在生理条件下,采用紫外吸收光谱法及荧光光谱法研究了PTP与牛血清白蛋白(BSA)的相互作用,并采用同步荧光法考察了PTP的加入对BSA构象的影响。结果表明,PTP对BSA的荧光猝灭机理为静态猝灭过程,PTP与BSA的结合反应为自发进行,反应中主要作用力是氢键和范德华力,两者的结合位点数为1、结合距离为1.78nm,PTP的加入对BSA构象没有明显影响。

Through Aza-Wittig reaction, 3-phenyl-2- （ 4-tert-butylphenoxy ）-pentamethyleneoxide [ 3＇, 4- 5,4 ] thieno [2,3-d] pyrimidin-4 （3 H）-one （PTP） was synthesized by cyclization of carbodiimide and phenolic com- pound under the conditions of alkaline catalysis. The interaction between PTP and bovine serum albumin （BSA） was investigated by fluorescence and UV absorption spectroscopy under physiological condition,and the effect of PTP on the conformation of BSA was analyzed via the synchronous fluorescence spectra. The results showed that PTP observably quenched the fluorescence of BSA in a static quenching mode,the binding reaction was spontaneous and the main binding forces were hydrogen binding and Van der Waals interaction,the number of binding site and the binding distance was 1 and 1.78 nm,respectively. And the addition of PTP didnft change the conformation of BSA.