有机化学 ›› 2014, Vol. 34 ›› Issue (7): 1452-1457.DOI: 10.6023/cjoc201401039 上一篇    下一篇

研究简报

多肽酰肼法合成Nesiritide

陈晨晨a, 李思践a, 陈轶群b, 许华建a, 李宜明a   

  1. a 合肥工业大学化学工程学院 医学工程学院 合肥 230009;
    b 安徽大学生命科学学院 合肥 230009
  • 收稿日期:2014-01-24 修回日期:2014-03-22 出版日期:2014-07-25 发布日期:2014-04-02
  • 通讯作者: 许华建, 李宜明 E-mail:lym2007@mail.ustc.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.21102083;21372058)资助项目.

Synthesis of Nesiritide via Ligation of Peptide Hydrazide

Chen Chenchena, Li Sijiana, Chen Yiqunb, Xu Huajiana, Li Yiminga   

  1. a School of Chemical Engineering, School of Medical Engineering, Hefei University of Technology, Hefei 230009;
    b School of Life Science, Anhui University, Hefei 230601
  • Received:2014-01-24 Revised:2014-03-22 Online:2014-07-25 Published:2014-04-02
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 201102083, 21372058).

Nesiritide是一类重要的多肽类血管扩张药物,在维持心血管和肾脏的体内平衡方面发挥着重要的作用. 目前,Nesiritide的合成主要是通过基因重组表达法获得,该方法操作较为复杂且存在一定的限制. 本研究运用多肽固相合成及酰肼连接策略,通过3片段连接高效合成了Nesiritide,为大批量工业化生产该类多肽药物打下基础.

关键词: 多肽酰肼连接, 自然化学连接, 多肽硫酯, Nesiritide

Nesiritide is an important class of peptide vasodilator. It plays a significant role in the maintenance homeostasis of cardiovascular and kidney. Nowadays, nesiritide is mainly obtained by biological methods including gene recombinant expression, which is relative time-consuming. In present work, the chemical synthesis of nesiritide was reported by using (solid-phase peptide synthesis) (SPPS) strategy combining with the ligation of peptide hydrazides with high yield and purity. Therefore, it was considered that the method presented here provided a convinced alternative for acquiring pharmaceutical peptide in a large scale.

Key words: ligation of peptide hydrazide, native chemical ligation, peptide thioester, nesiritide