降糖多肽CW7213的合成制备研究  

The Preparation and Synthesis of CW7213

作　　者：孔毅[1] 赖伊丽[1] 黄海[1] 颜天华[1] 

机构地区：[1]中国药科大学生命科学与技术学院,南京210009

出　　处：《药物生物技术》2012年第5期397-400,共4页Pharmaceutical Biotechnology

基　　金：重大新药创制(No.2009ZX09103-091)

摘　　要：CW7213是胰高血糖素样肽-1(GLP-1)类似物,具有多种生理功能:能够降低患者体重,更平稳地控制血糖水平,不会产生低血糖。该文主要对CW7213合成方法进行研究:以Fmoc-Gly-WANG树脂为起始原料,以HBTU、TBTU/HOBt为缩合剂,对长肽的合成方法和活性较低氨基酸的缩合方法进行优化。采用制备型反相高效液相色谱仪优化了CW7213的纯化方法。采用HPLC对产品进行了纯度分析,采用MS测定了其分子量。得到的CW7213纯度高达98.8%,总收率为21.3%。该方法简单易行,所得产品纯度和收率较高,能够满足CW7213药效学和毒理研究的需要。CW7213 is an analog of Glucagon-Like Peptide-1 （GLP-1）. It has various physiological functions,including lowering the body weight and balancing the blood sugar level,but not lead to hypoglycemia. This article focuses on the synthesis of CW7213. The CW7213 with Fmoc Solid phase peptide synthesis was firstly synthesized. The related issues in the synthesis technology were studied. Fmoc-Gly-WANG resin was used as the vector ,HBTU and TBTU as the coupling agents. The coupling reaction paravaeters of the low activity amino acids were optimized. The purification of CW7213 was conducted with semi-preparative HPLC-Bio-Rad, and several chromatographic parameters were optimized too. The purity of the product was analyzed by HPLC and the molecule weight was determined by MALDI-TOF MS . The purity of the refined peptide was 98.8% and the overall yield was 21.3%. It is the first report that the CW7213, a novel analog of GLP-1, was synthesized. The synthesis method of CW7213 is simple and feasible. It can meet the need of studying pharmaeodynamies and toxicology of CW7213.

关 键 词：CW7213 固相合成 GLP-1 糖尿病 Fmoc法 

分 类 号：TQ464.7[化学工程—制药化工]