高等学校化学学报

高等学校化学学报 ›› 2004, Vol. 25 ›› Issue (10): 1853.

• 研究论文 • 上一篇    下一篇

酶催化法合成CCK-8的一个四肽片段

项光亚1, 吕子敏1, HeinerEckstein2   

  1. 1. 华中科技大学同济医学院药学院, 武汉430030;
    2. 德国蒂宾根大学有机化学研究所, 蒂宾根72076
  • 收稿日期:2003-07-10 出版日期:2004-10-24 发布日期:2004-10-24
  • 基金资助:

    国家自然科学基金(批准号:30300430);留学回国人员科研启动基金(批准号:2003-406);武汉市晨光计划(批准号:2001-103)资助

Synthesis of a CCK-8 Tetrapeptide Fragment by Enzyme-catalyzed Method

XIANG Guang-Ya1, LÜ Zi-Min1, HEINER Eckstein2   

  1. 1. Pharmacy School of Tongji Medical College, Huazhong University of Science & Technology, Wuhan 430030, China;
    2. Institute of Organic Chemistry, University of Tuebingen, Tuebingen 72076, Germany
  • Received:2003-07-10 Online:2004-10-24 Published:2004-10-24

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被引次数

5

摘要： 用酶催化法合成了缩胆囊素(CCK-8)的1个四肽片段(Phac-Met-Gly-Trp-Met-OEt).该四肽片段是依次通过Phac-Met-OEt与Gly-OMe·HCl,Trp-OMe和Met-OEt偶合得到的,这3步偶合反应分别用α-糜蛋白酶、木瓜蛋白酶和α-糜蛋白酶作为催化剂,并对影响反应的因素进行了研究,反应中间体和产物均经质谱(FAB-MS)分析证实.

关键词: 缩胆囊素(CCK-8), 酶催化法, &alpha, -糜蛋白酶, 木瓜蛋白酶

Abstract: Cholecystokinin(CCK) is a polypeptide hormones with gastrointestinal, biliar and brain activities. Many methods were reported on the synthesis of the C-terminal octapeptide. Enzymatic techeiques possess numerous advantages over chemical techniques for the formation of the peptide bond. Here we reported an enzyme-catalyzed method to synthesize a cholecystokinin tetrapeptide(Phac-Met-Gly-Trp-Met-OEt) fragment. It was synthesized by coupling Phac-Met-OEt with Gly-OMe·HCl, Trp-OMe and Met-OEt successively, these three steps were catalyzed by α-chymotrpsin, papain and α-chymotrpsin respectively. The influence factors on the reaction including the choice of enzymes, solvents, acyl donor and buffer contents were also studied. All the reaction intermediates and products were confirmed to have the correct molecular mass by the results of FAB-MS.

Key words: CCK-8, Enzyme-catalyzed method, α-Chymotrpsin, Papain

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