[12]aneN3-based lipid with naphthalimide moiety for enhanced gene transfection efficiency

Bioorg Chem. 2018 Sep:79:334-340. doi: 10.1016/j.bioorg.2018.04.018. Epub 2018 May 3.

Abstract

Three cationic lipids derived from [12]aneN3 modified with naphthalimide (1a), oleic acid (1b) and octadecylamine (1c) were designed and synthesized. In vitro transfection showed that all these liposomes can deliver plasmid DNA into the tested cell lines. Among these liposomes, 1a gave the best transfection efficiency (TE) in A549 cells, which was higher than that of lipofectamine 2000. More importantly, the TE of 1a was dramatically increased in the presence of 10% serum. These results suggested that 1a might be a promising non-viral gene vector, and also give further insight for developing novel high performance gene delivery agents.

Keywords: Cationic lipids; Naphthalimide; Non-viral vectors; Transfection efficiency; [12]aneN3.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Gene Transfer Techniques*
  • Humans
  • Lipids / chemistry*
  • Lipids / pharmacology
  • Luciferases / genetics*
  • Luciferases / metabolism
  • Molecular Structure
  • Naphthalimides / chemistry*
  • Naphthalimides / pharmacology
  • Structure-Activity Relationship
  • Transfection

Substances

  • Lipids
  • Naphthalimides
  • Luciferases