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Cyclen-Based Cationic Lipids Containing Carbamate Linkages as Efficient Gene Delivery Vectors with Low Toxicity

  1. Dr. Qing-Dong Huang1,†,
  2. Jiang Ren1,†,
  3. Hong Chen1,2,
  4. Wen-Jing Ou1,
  5. Dr. Ji Zhang1,*,
  6. Yun Fu1,
  7. Prof. Dr. Wen Zhu1,*,
  8. Prof. Dr. Xiao-Qi Yu1,*

Article first published online: 31 MAY 2012

DOI: 10.1002/cplu.201200060

Issue

ChemPlusChem

ChemPlusChem

Volume 77, Issue 7, pages 584–591, July 2012

Additional Information

How to Cite

Huang, Q.-D., Ren, J., Chen, H., Ou, W.-J., Zhang, J., Fu, Y., Zhu, W. and Yu, X.-Q. (2012), Cyclen-Based Cationic Lipids Containing Carbamate Linkages as Efficient Gene Delivery Vectors with Low Toxicity. ChemPlusChem, 77: 584–591. doi: 10.1002/cplu.201200060

Author Information

  1. 1

    Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610064 (P. R. China)

  2. 2

    Department of Basic Science, Rongchang Campus, Southwest China University, Chongqing 402460 (P. R. China)

  1. †

    These authors contributed equally to this work.

*Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610064 (P. R. China)

  1. †

    These authors contributed equally to this work.

Publication History

  1. Issue published online: 5 JUL 2012
  2. Article first published online: 31 MAY 2012
  3. Manuscript Revised: 15 MAY 2012
  4. Manuscript Received: 17 MAR 2012

Funded by

  • National Science Foundation of China. Grant Numbers: 20972104, 20902062, 2012CB720603
  • Analytical & Testing Center of Sichuan University

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Keywords:

  • carbamates;
  • cationic lipids;
  • cyclen;
  • gene delivery;
  • nonviral vectors

Abstract

Two novel cationic lipids based on protonated cyclen and steroid (cholesterol or diosgenin) moieties with carbamate linkage have been designed and synthesized for gene delivery. Cationic liposomes were easily prepared from each of these lipids individually or from the mixtures of each cationic lipid and dioleoylphosphatidyl ethanolamine (DOPE). Several studies including dynamic light scattering, gel retardation assay, ethidium bromide intercalation assay, and transmission electron microscopy (TEM) imaging demonstrate that these amphiphilic molecules are able to bind and compact DNA into nanoparticles which may act as nonviral gene delivery agents. Results from in vitro transfection show that in association with (DOPE), two cationic lipids can induce effective gene transfection in HEK 293, A549, and H460 cells. Especially, in tumor cells (A549 and H460), the gene transfection efficiency of two cationic lipids were found to be higher than that of commercially available Lipofectamine 2000. The lipoplexes formed from both cationic lipids were found to have low cytotoxicity in three cell lines even at high N/P ratios.

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