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

• Published in: Chemical communications (Cambridge, England) Vol. 56; no. 89; pp. 13796 - 13799
• Main Authors: Xin, Pengyang, Zhao, Lingyu, Mao, Linlin, Xu, Linqi, Hou, Shuaimin, Kong, Huiyuan, Fang, Haodong, Zhu, Haofeng, Jiang, Tao, Chen, Chang-Po
• Format: Journal Article
• Language: English
• Published: England Royal Society of Chemistry 18.11.2020
• Subjects: Animals; Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Antibiotics; Antiinfectives and antibacterials; Antimicrobial agents; antimicrobial properties; Bacillus subtilis - drug effects; Calixarenes - chemistry; Calixarenes - pharmacology; Channels; Dose-Response Relationship, Drug; Erythrocytes - drug effects; Gramicidin - chemistry; Gramicidin - pharmacology; Ion Channels - antagonists & inhibitors; Ion Channels - metabolism; Ion transport; Ion Transport - drug effects; Ions; mammals; Microbial Sensitivity Tests; Microorganisms; Molecular Structure; NMR; Nuclear magnetic resonance; peptides; Rats; Staphylococcus aureus - drug effects; Toxicity
• ISSN: 1359-7345; 1364-548X; 1364-548X
• DOI: 10.1039/d0cc05730d

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 (IC 50 = 0.55 μM) and negligible hemolytic toxicity, showing potential to serve as a systemic antibiotic. The charge status of channels formed by pillararene-gramicidin hybrid molecules has a significant impact on their trans-membrane transport properties, membrane-association abilities and antimicrobial activities.