Exploiting Macromolecular Design To Optimize the Antibacterial Activity of Alkylated Cationic Oligomers

Biomacromolecules. 2018 Dec 10;19(12):4629-4640. doi: 10.1021/acs.biomac.8b01317. Epub 2018 Nov 6.

Abstract

There is growing interest in synthetic polymers which co-opt the structural features of naturally occurring antimicrobial peptides. However, our understanding of how macromolecular architecture affects antibacterial activity remains limited. To address this, we investigated whether varying architectures of a series of block and statistical co-oligomers influenced antibacterial and hemolytic activity. Cu(0)-mediated polymerization was used to synthesize oligomers constituting 2-(Boc-amino)ethyl acrylate units and either diethylene glycol ethyl ether acrylate (DEGEEA) or poly(ethylene glycol) methyl ether acrylate units with varying macromolecular architecture; subsequent deprotection produced primary amine functional oligomers. Further guanylation provided an additional series of antimicrobial candidates. Both chemical composition and macromolecular architecture were shown to affect antimicrobial activity. A broad spectrum antibacterial oligomer (containing guanidine moieties and DEGEEA units) was identified that possessed promising activity (MIC = 2 μg mL-1) toward both Gram-negative and Gram-positive bacteria. Bacterial membrane permeabilization was identified as an important contributor to the mechanism of action.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylates / chemistry
  • Acrylates / pharmacology
  • Alkylating Agents / chemistry*
  • Alkylating Agents / pharmacology
  • Alkylation
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology
  • Antimicrobial Cationic Peptides / chemistry*
  • Antimicrobial Cationic Peptides / pharmacology
  • Cations / chemistry
  • Cations / pharmacology
  • Macromolecular Substances / chemistry
  • Macromolecular Substances / pharmacology
  • Microbial Sensitivity Tests
  • Molecular Structure*
  • Polymerization / drug effects
  • Polymers / chemistry
  • Structure-Activity Relationship

Substances

  • Acrylates
  • Alkylating Agents
  • Anti-Bacterial Agents
  • Antimicrobial Cationic Peptides
  • Cations
  • Macromolecular Substances
  • Polymers
  • ethyl acrylate
  • methyl acrylate