天然产物研究与开发 ›› 2018, Vol. 30 ›› Issue (12): 2203-2206.doi: 10.16333/j.1001-6880.2018.12.026

• 开发研究 • 上一篇    下一篇

芋螺毒素ImI的化学合成及其杀虫活性研究

吴小英1,安婷婷2,高炳淼3*   

  1. 1海南省人民医院;2海南省药物研究所,海口 570311;3海南医学院,海口 571199
  • 出版日期:2019-01-02 发布日期:2019-01-02
  • 基金资助:

    海南省重点研发计划(ZDYF2018138);国家自然科学基金(81560611)

Chemical Synthesis and Insecticidal Activity of Conotoxin ImI

WU Xiao-ying1, AN Ting-ting2, GAO Bing-miao3*   

  1. 1Hainan General Hospital; 2Pharmaceutical Institute of Hainan Province,Haikou 570311,China; 3Hainan Medical University,Haikou 571199,China  
  • Online:2019-01-02 Published:2019-01-02

摘要: 为研究芋螺毒素ImI的杀虫活性,本研究采用化学方法合成芋螺毒素线性肽,经氧化折叠后质谱鉴定获得芋螺毒素ImI,采用MTT法和昆虫注射法研究其杀虫活性。结果表明采用化学合成法可以成功合成芋螺毒素线性肽,经氧化折叠后质谱鉴定形成2个二硫键;活性实验表明芋螺毒素ImI具有抑制昆虫细胞sf9生长的活性,半数有效量为0.13 nM;对黄粉虫具有杀虫活性,半数致死剂量为0.11 μg/mg。通过化学合成法可以有效合成芋螺毒素ImI,其具有良好的杀虫活性,可为研发新型多肽类生物杀虫剂奠定基础。

关键词: 芋螺毒素, 化学合成, 氧化折叠, 杀虫活性

Abstract: To study insecticidal activity of Conotoxin ImI,the conotoxin linear peptide was synthesized by chemical method,and conotoxin ImI was identified by mass spectrometry after oxidative folding.The insecticidal activity of conotoxin was evaluated by MTT method and insect injection method.The results show that conotoxins linear peptides were successfully synthesized by chemical synthesis method,and two disulfide bonds were identified by mass spectrometry after oxidative folding.The activity test showed conotoxin ImI could inhibit the growth of sf9 in insect cells,and the half effective dose was 0.13 nM.It had a killing effect on Tenebrio molitor,with a median lethal dose was 0.11 μg/mg.Therefore,the conotoxin ImI can be synthesized by chemical synthesis,which has the insecticidal activity and can lay the foundation for the development of new peptide bio-pesticides.

Key words: conotoxin, chemical synthesis, oxidative folding, insecticidal activity

中图分类号: 

R931