The antimicrobial effects of the alginate oligomer OligoG CF-5/20 are independent of direct bacterial cell membrane disruption

Sci Rep. 2017 Mar 31:7:44731. doi: 10.1038/srep44731.

Abstract

Concerns about acquisition of antibiotic resistance have led to increasing demand for new antimicrobial therapies. OligoG CF-5/20 is an alginate oligosaccharide previously shown to have antimicrobial and antibiotic potentiating activity. We investigated the structural modification of the bacterial cell wall by OligoG CF-5/20 and its effect on membrane permeability. Binding of OligoG CF-5/20 to the bacterial cell surface was demonstrated in Gram-negative bacteria. Permeability assays revealed that OligoG CF-5/20 had virtually no membrane-perturbing effects. Lipopolysaccharide (LPS) surface charge and aggregation were unaltered in the presence of OligoG CF-5/20. Small angle neutron scattering and circular dichroism spectroscopy showed no substantial change to the structure of LPS in the presence of OligoG CF-5/20, however, isothermal titration calorimetry demonstrated a weak calcium-mediated interaction. Metabolomic analysis confirmed no change in cellular metabolic response to a range of osmolytes when treated with OligoG CF-5/20. This data shows that, although weak interactions occur between LPS and OligoG CF-5/20 in the presence of calcium, the antimicrobial effects of OligoG CF-5/20 are not related to the induction of structural alterations in the LPS or cell permeability. These results suggest a novel mechanism of action that may avoid the common route in acquisition of resistance via LPS structural modification.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alginates / chemistry
  • Alginates / pharmacology*
  • Anti-Infective Agents / pharmacology*
  • Cations, Divalent / pharmacology
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism*
  • Cell Membrane Permeability / drug effects
  • Cell Wall / drug effects
  • Cell Wall / metabolism
  • Glucuronic Acid / chemistry
  • Glucuronic Acid / pharmacology
  • Hexuronic Acids / chemistry
  • Hexuronic Acids / pharmacology
  • Lipopolysaccharides / chemistry
  • Lipopolysaccharides / pharmacology
  • Microbial Sensitivity Tests
  • Pseudomonas aeruginosa / cytology*
  • Pseudomonas aeruginosa / drug effects
  • Streptococcus mutans / cytology*
  • Streptococcus mutans / drug effects

Substances

  • Alginates
  • Anti-Infective Agents
  • Cations, Divalent
  • Hexuronic Acids
  • Lipopolysaccharides
  • Glucuronic Acid