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

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.