Synthesis of lipid-oligonucleotide conjugates for RNA interference studies

Chem Biodivers. 2011 Feb;8(2):287-99. doi: 10.1002/cbdv.201000274.

Abstract

The synthesis of RNA molecules carrying lipids at their 3'-termini and 5'-termini is reported. These conjugates were fully characterized by MALDI-TOF mass spectrometry and HPLC chromatography. The ability of these conjugates to silence gene expression was evaluated in the inhibition of the tumor necrosis factor. All the lipid-siRNA derivatives were compatible with RNA interference machinery if transfected with oligofectamine. In the absence of a transfection agent, some lipid-siRNA derivatives can exert a slight reduction of gene expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Chromatography, High Pressure Liquid
  • Enzyme-Linked Immunosorbent Assay
  • Gene Expression / drug effects
  • HeLa Cells
  • Humans
  • Lipids / chemistry*
  • Mice
  • Molecular Targeted Therapy / methods
  • Oligonucleotides / chemical synthesis*
  • Oligonucleotides / genetics
  • Oligonucleotides / pharmacology
  • RNA Interference*
  • RNA, Small Interfering / chemical synthesis*
  • RNA, Small Interfering / genetics
  • RNA, Small Interfering / pharmacology
  • Recombinant Proteins / antagonists & inhibitors*
  • Recombinant Proteins / biosynthesis
  • Recombinant Proteins / genetics
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
  • Transfection
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors*
  • Tumor Necrosis Factor-alpha / biosynthesis
  • Tumor Necrosis Factor-alpha / genetics

Substances

  • Lipids
  • Oligonucleotides
  • RNA, Small Interfering
  • Recombinant Proteins
  • Tumor Necrosis Factor-alpha
  • oligofectamine