Host Defense Peptide-Mimicking Amphiphilic β-Peptide Polymer (Bu:DM) Exhibiting Anti-Biofilm, Immunomodulatory, and in Vivo Anti-Infective Activity

J Med Chem. 2020 Nov 12;63(21):12921-12928. doi: 10.1021/acs.jmedchem.0c01321. Epub 2020 Oct 30.

Abstract

Therapeutic options to treat multidrug resistant bacteria, especially when present in biofilms, are limited due to their high levels of antibiotic resistance. Here, we report the anti-biofilm and immunomodulatory activities of the host defense peptide (HDP)-mimicking β-peptide polymer (20:80 Bu:DM) and investigated its activity in vivo. The polymer outperformed antibiotics in the removal and reduction of the viability of established biofilms, achieving a maximum activity of around 80% reduction in viability. Interestingly the polymer also exhibited HDP-like immunomodulation in inducing chemokines and anti-inflammatory cytokines and suppressing lipopolysaccharide-induced proinflammatory cytokines. When tested in a murine, high-density skin infection model using P. aeruginosa LESB58, the polymer was effective in diminishing abscess size and reducing bacterial load. This study demonstrates the dual functionality of HDP-mimicking β-peptide polymers in inhibiting biofilms and modulating innate immunity, as well as reducing tissue dermonecrosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / pharmacology
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Anti-Infective Agents / therapeutic use
  • Antimicrobial Cationic Peptides / chemistry*
  • Biofilms / drug effects*
  • Cell Survival / drug effects
  • Cytokines / pharmacology
  • Disease Models, Animal
  • Humans
  • Immunity, Innate / drug effects
  • Leukocytes, Mononuclear / cytology
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / metabolism
  • Methicillin-Resistant Staphylococcus aureus
  • Microbial Sensitivity Tests
  • Peptidomimetics
  • Polymers / chemistry*
  • Polymers / pharmacology
  • Polymers / therapeutic use
  • Pseudomonas aeruginosa / drug effects
  • Pseudomonas aeruginosa / physiology
  • Skin Diseases / drug therapy
  • Skin Diseases / microbiology
  • Skin Diseases / pathology

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Antimicrobial Cationic Peptides
  • Cytokines
  • Peptidomimetics
  • Polymers

Grants and funding