Amphiphilic Polymethyloxazoline-Polyethyleneimine Copolymers: Interaction with Lipid Bilayer and Antibacterial Properties

Macromol Biosci. 2019 Dec;19(12):e1900254. doi: 10.1002/mabi.201900254. Epub 2019 Nov 20.

Abstract

Polycations, mimicking activity of antibacterial peptides, belong to an important class of molecules investigated as a support or as an alternative to antibiotics. In this work, studies of modified linear amphiphilic statistical polymethyloxazoline (PMOX) and polyethyleneimine copolymers (PMOX_PEI) series are presented. Variation of PEI content in the structure results in controllable changes of polymeric aggregates zeta potential. The structure with the highest positive charge shows the best antimicrobial activity, well visible in tests against model Gram-positive and Gram-negative bacteria, fungi, and mycobacterium strains. The polymer toxicity is evaluated with MTT and hemolysis assay as a reference. Quartz crystal microbalance (QCM-D) is used to investigate interaction between polycations and a model lipid membrane. Polymer activity correlates well with molecular structure, showing that amphiphilic component is altering polymer behavior in contact with the lipid bilayer.

Keywords: antimicrobial properties; backbone charged polycations; model membranes; zeta potential.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemical synthesis
  • Anti-Infective Agents / pharmacology*
  • Antimicrobial Cationic Peptides / chemistry
  • Candida albicans / drug effects
  • Candida albicans / growth & development
  • Erythrocytes / drug effects
  • Escherichia coli / drug effects
  • Escherichia coli / growth & development
  • Hemolysis / drug effects
  • Humans
  • Lipid Bilayers / chemistry*
  • Microbial Sensitivity Tests
  • Molecular Mimicry
  • Molecular Structure
  • Mycobacterium avium / drug effects
  • Mycobacterium avium / growth & development
  • Mycobacterium bovis / drug effects
  • Mycobacterium bovis / growth & development
  • Mycobacterium tuberculosis / drug effects
  • Mycobacterium tuberculosis / growth & development
  • Nontuberculous Mycobacteria / drug effects
  • Nontuberculous Mycobacteria / growth & development
  • Polyamines / chemical synthesis
  • Polyamines / pharmacology*
  • Polyelectrolytes / chemistry
  • Polyethyleneimine / chemical synthesis
  • Polyethyleneimine / pharmacology*
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / growth & development
  • Static Electricity
  • Structure-Activity Relationship

Substances

  • Anti-Infective Agents
  • Antimicrobial Cationic Peptides
  • Lipid Bilayers
  • Polyamines
  • Polyelectrolytes
  • poly(2-methyloxazoline)
  • polycations
  • Polyethyleneimine