Effect of charge status on the ion transport and antimicrobial activity of synthetic channels

Chem Commun (Camb). 2020 Nov 18;56(89):13796-13799. doi: 10.1039/d0cc05730d. Epub 2020 Oct 20.

Abstract

A class of unimolecular channels formed by pillararene-gramicidin hybrid molecules are presented. The charge status of the peptide domain in these channels has a significant impact on their ion transport and antimicrobial activity. These channels exhibited different membrane-association abilities between microbial cells and mammalian cells. One of the channels displayed a higher antimicrobial activity towards S. aureus (IC50 = 0.55 μM) and negligible hemolytic toxicity, showing potential to serve as a systemic antibiotic.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacillus subtilis / drug effects*
  • Calixarenes / chemistry
  • Calixarenes / pharmacology*
  • Dose-Response Relationship, Drug
  • Erythrocytes / drug effects
  • Gramicidin / chemistry
  • Gramicidin / pharmacology*
  • Ion Channels / antagonists & inhibitors*
  • Ion Channels / metabolism
  • Ion Transport / drug effects
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Rats
  • Staphylococcus aureus / drug effects*

Substances

  • Anti-Bacterial Agents
  • Ion Channels
  • Calixarenes
  • Gramicidin