Lipid oligonucleotides as a new strategy for tackling the antibiotic resistance

Sci Rep. 2020 Jan 23;10(1):1054. doi: 10.1038/s41598-020-58047-x.

Abstract

Antibiotic resistance has become a major issue in public health especially for one of the most used antibiotics; the third-generation cephalosporins. One of the main resistance mechanisms in Enterobacteriaceae, is the production of Extended-Spectrum β-lactamases. Here, we demonstrated that the oligonucleotide therapy is an efficient approach to reduce the resistance of bacteria to antibiotic treatment. Lipid oligonucleotides (LONs) were proved to be efficient strategies in both delivering the oligonucleotide sequences in the prokaryotic cells and decreasing the Minimum Inhibitory Concentration of resistant bacteria to a third generation cephalosporin, the ceftriaxone. Accordingly, we demonstrated the strong antimicrobial potential of this LON strategy targeting the ß-lactamase activity on both clinical and laboratory strains. Our results support the concept that the self-delivery of oligonucleotide sequences via lipid conjugation may be extended to other antimicrobial drugs, which opens novel ways to struggle against the antibiotic resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Ceftriaxone / pharmacology*
  • Cephalosporins / pharmacology
  • Drug Carriers / chemistry*
  • Drug Resistance, Bacterial / genetics*
  • Escherichia coli / drug effects*
  • Escherichia coli / genetics
  • Escherichia coli Infections / drug therapy
  • Escherichia coli Infections / microbiology
  • Escherichia coli Proteins / genetics
  • Humans
  • Lipids / chemistry
  • Microbial Sensitivity Tests
  • Oligonucleotides / chemistry*
  • beta-Lactamases / genetics

Substances

  • Anti-Bacterial Agents
  • Cephalosporins
  • Drug Carriers
  • Escherichia coli Proteins
  • Lipids
  • Oligonucleotides
  • Ceftriaxone
  • beta-Lactamases
  • beta-lactamase CTX-M, E coli