Spacer structure and hydrophobicity influences transfection activity of novel polycationic gemini amphiphiles

Bioorg Med Chem Lett. 2017 Aug 1;27(15):3284-3288. doi: 10.1016/j.bmcl.2017.06.026. Epub 2017 Jun 10.

Abstract

Three novel polycationic gemini amphiphiles with different spacers were developed and evaluated in terms of their physiochemical properties and transfection efficiencies. Cationic liposomes formed by these amphiphiles and the helper lipid DOPE were able to successfully condense DNA, as shown by gel mobility shift and ethidium bromide intercalation assays. Transfection activity of the liposomes was superior to Lipofectamine® 2000 and was dependent on spacer structure, hydrophobicity, and nucleic acid type (pDNA or siRNA). We demonstrated that the cationic liposomes 2X6/DOPE and 2X7/DOPE are potential non-toxic vehicles for gene delivery.

Keywords: Cationic liposomes; Gemini amphiphiles; Gene therapy; Spacer; Transfection.

MeSH terms

  • DNA / administration & dosage*
  • DNA / genetics
  • HEK293 Cells
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Lipids / chemistry
  • Liposomes / chemistry
  • Phosphatidylethanolamines / chemistry
  • Plasmids / administration & dosage*
  • Plasmids / genetics
  • Polyamines / chemistry*
  • Polyelectrolytes
  • RNA, Small Interfering / administration & dosage*
  • RNA, Small Interfering / genetics
  • Surface-Active Agents / chemistry*
  • Transfection / methods*

Substances

  • Lipids
  • Lipofectamine
  • Liposomes
  • Phosphatidylethanolamines
  • Polyamines
  • Polyelectrolytes
  • RNA, Small Interfering
  • Surface-Active Agents
  • polycations
  • dioleoyl phosphatidylethanolamine
  • DNA