清除血浆中LDL用短肽SDE的合成研究  

Synthesis of SDE Tripeptide for Eliminating LDL in Plasma

作　　者：许映霞[1] 万昌秀[1] 姚红卫[1] 黄小华[1] 乐以伦[1] 

机构地区：[1]四川大学高分子材料与工程学院,四川成都610065

出　　处：《四川大学学报（工程科学版）》2002年第3期65-68,共4页Journal of Sichuan University (Engineering Science Edition)

基　　金：国家自然科学基金资助项目 (2 98740 2 2 )

摘　　要：采用DCC/HOBt液相法先将BOC -Asp(OBzL)和Glu(OBzL) 2 偶合反应生成DE二肽 ,再将此二肽与Z -Ser- (Bzl)反应 ,合成具有生物活性的Ser-Asp -Glu三肽 (SDE) ,此三肽对血浆中低密度脂蛋白 (LDL)的识别及特异性吸附起关键性作用。研究反应温度、反应时间和原料配比对二肽DE和三肽SDE产率的影响 ,通过正交实验优化实验方案 ,得到合成二肽的最优方案为 :- 5℃ ,8h ,原料配比Asp∶DCC为 1∶1.0 8;合成SDE的最优条件为 :- 5℃ ,12h ,原料配比Ser∶DCC为 1∶1.0 8。SDE经纯化后 。A Ser-Asp-Glu tripeptide (SDE) which can specially recognize and bind LDL in blood was prepared. For the preparation of SDE, the Asp-Glu dipeptide (DE) was first synthesized by coupling BOC-Asp(OBzL) with Glu(OBzL ) 2, and then coupled with Z-Ser-(BzL) by means of the carbodiimide method. The effects of temperature, time and the ratio of materials on the yield of the synthesis were studied by the ortho design method. The optimal synthesis conditions of DE dipeptide and SDE tripeptide are -5?℃,8?h,Asp∶DCC=1∶1.08 and -5?℃,12?h,Ser∶DCC=1∶1.08 respectively . After deprotected by catalytic hydrogenolysis and purified by chromatography, the SDE tripeptide was evaluated by mass spectra and amino acid analyzing spectra. The results showed that the tripeptide was synthesized successfully.

关 键 词：血浆 LDL 短肽SDE Ser-Asp-Glu三肽 低密度指蛋白 液相合成 高脂血症 血液净化法 冠心病 

分 类 号：R541.4[医药卫生—心血管疾病]