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Exendin-4的固相化学合成及鉴定
引用本文:刘延杰,季虹,林鲁霞,臧学章,宋长征,荣海钦.Exendin-4的固相化学合成及鉴定[J].中国生物工程杂志,2011,31(2):69-73.
作者姓名:刘延杰  季虹  林鲁霞  臧学章  宋长征  荣海钦
作者单位:山东省内分泌与代谢病研究所 山东省医学科学院 济南 250062
基金项目:山东省科技攻关计划(2009GG20002046、2009GG20002049)资助项目
摘    要:Exendin-4是首个获准上市的肠促胰素类似物药物,可模拟人体自身激素GLP-1的功能,不仅改善血糖,还能促进胰岛β细胞新生、增殖,抑制β细胞凋亡,改善β细胞功能,促进胰岛素分泌,增加机体对胰岛素的敏感性。根据Exendin-4的潜在市场价值,以Fmoc固相合成策略为基础,NMP为反应溶剂,以HOBt/DIC为缩合剂,添加盖帽程序,优化合成工艺条件。肽树脂裂解采用TFA/Phenol/TIS裂解液,并应用高效液相色谱和四级杆-飞行时间串联质谱对其进行分析鉴定和纯化,最终获得Exendin-4,产率为21%,纯度为99.4%。活性测定结果显示,合成的Exendin-4显著提高胰岛瘤细胞的活性,并呈一定剂量依赖性。

关 键 词:Exendin-4  固相化学合成  2型糖尿病  
收稿时间:2010-11-02
修稿时间:2010-11-29

Solid Phase Peptide Syntehesis and Analysis for Exendin-4
LIU Yan-jie,JI Hong,LIN Lu-xia,ZANG Xue-zhang,SONG Chang-zheng,RONG Hai-qin.Solid Phase Peptide Syntehesis and Analysis for Exendin-4[J].China Biotechnology,2011,31(2):69-73.
Authors:LIU Yan-jie  JI Hong  LIN Lu-xia  ZANG Xue-zhang  SONG Chang-zheng  RONG Hai-qin
Institution:LIU Yan-jie JI Hong LIN Lu-xia ZANG Xue-zhang SONG Chang-zheng RONG Hai-qin(Shandong Institute of Endocrine and Metabolic Diseases,Shandong Academy of Medical Science,Jinan 250062,China)
Abstract:Exendin-4 is the first-approved drug of the incretin mimetic family, which acts like the naturally occurring hormone GLP-1 in vivo. Exendin-4 decreases fasting and postprandial plasma glucose levels. Exendin-4 may play a role in enhancing glucose-dependent stimulation of insulin secretion, and maintaining of β-cell mass by promotion of β-cell proliferation and neogenesis, and inhibiting of β-cell apoptosis. This experiment studied the standard Fmoc strategy solid phase synthesis of Exendin-4. Using NMP as the coupling solvent, HOBt/DIC as the coupling reagent, AIM as the containing reagent. Synthesized peptides were clearaged by TFA/Phenol/TIS, and identified by high performance liquid chromatography and quadrupole time of flight LC/MS. The yield of pure Exendin-4 was 21% with a purity of 99.4%. Using the SRB method to measure the bioassay of Exendin-4 cell regeneration experiment. It is an influential research into the therapy of type 2 diabetes mellitus.
Keywords:Exendin-4 Solid phase peptide synthesis Type 2 diabetes mellitus  
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