高等学校化学学报 ›› 2011, Vol. 32 ›› Issue (9): 2157.

• 研究论文 • 上一篇    下一篇

含双Cyclen阳离子脂质的合成及与DNA的相互作用

陈红1,2,廖易乐1,黄清东1,吴江1,余孝其1   

  1. 1. 四川大学化学学院, 绿色化学与技术教育部重点实验室, 成都 610064;
    2. 西南大学荣昌校区基础部, 重庆 402460
  • 收稿日期:2011-01-24 修回日期:2011-05-27 出版日期:2011-09-10 发布日期:2011-08-11
  • 通讯作者: 余孝其;吴江 E-mail:xqyu@tfol.com;wujiang@scu.edu.cn
  • 基金资助:

    国家自然科学基金(批准号: 20972104, 20725206, 20732004)资助.

Synthesis of Cationic Lipids Containing Bis\|cyclen Units and Interaction with DNA

CHEN Hong1,2, LIAO Yi-Le1, HUANG Qing-Dong1, WU Jiang1*, YU Xiao-Qi1*   

  1. 1. Key Laboratory of Green Chemistry and Technology, Ministry of Education, College of Chemistry, Sichuan University, Chengdu 610064, China; 
    2. Department of Basic Sciences, Rongchang Campus, Southwest China University, Chongqing 402460, China
  • Received:2011-01-24 Revised:2011-05-27 Online:2011-09-10 Published:2011-08-11
  • Contact: YU Xiao-Qi;WU Jiang E-mail:xqyu@tfol.com;wujiang@scu.edu.cn
  • Supported by:

    国家自然科学基金(批准号: 20972104, 20725206, 20732004)资助.

摘要: 阳离子脂质体作为一类非常重要的基因转染载体正得到广泛的重视和研究. 本文设计合成了一类新型的阳离子脂质小分子化合物. 化合物1含有双cyclen亲水端和甾体疏水基团. 凝胶电泳实验显示含胆固醇和皂素的双大环多胺阳离子脂质与DOPE形成的阳离子脂质体能够与DNA有效作用, 在氮磷比为6时即可完全包裹DNA, 具备了作为非病毒基因载体的潜在性, 可为设计新型阳离子脂质基因载体提供了新思路.

关键词: 大环多胺, 合成, 阳离子脂质, 基因载体

Abstract: The clinical success of gene therapy requires a safe and effective gene delivery system. Cationic lipids have particularly excellent potential for gene delivery applications because of their lesser immunogenic nature, robust manufacture ability to deliver large pieces of DNA, and ease of handling and preparation techniques. In this study, two bis-cyclen-based cationic lipids were designed and synthesized, and their structures were characterized by 1H NMR and HRMS. Liposomes were easily prepared by mixing cationic lipids with DOPE. Agarose gel electrophoresis demonstrated that the liposomes could completely condense DNA at N/P ratio of 6. The results suggested that the synthesized cationic lipids might be of potential as non-viral gene carrier.

Key words: Cyclen, Synthesis, Cationic lipid, Gene vector

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