Lipoic acid modified antimicrobial peptide with enhanced antimicrobial properties. Issue 19 (1st October 2020)

• Record Type: Journal Article
• Authors: Zhou, Wenya; Du, Yawei; Li, Xinsong; Yao, Chen
• Is Part Of: Bioorganic & medicinal chemistry. Volume 28:Issue 19(2020)
• Publication Date: 2020-10-01
• Subjects: Antimicrobial peptide -- Bac8c -- Lipoic acid -- Membrane depolarization -- Membrane permeability -- Antibiofilm activity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2020.115682
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: RIWVIWRR-NH2 (Bac8c) is a natural antimicrobial peptide (AMP) exhibiting great antibacterial activity against Gram-negative and Gram-positive bacteria. In this work, lipoic acid was used as a fatty acid hydrophobic ligand to modify Bac8c (LA-Bac8c) to further improve its antimicrobial properties. Minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) assays showed that LA-Bac8c exhibited lower MIC (MBC) values against Staphylococcus aureus ( S. aureus ) and methicillin-resistant Staphylococcus aureus ( MRSA ) than Bac8c. Similar results were reflected in the antibiofilm activity towards S. aureus and MRSA, and LA-Bac8c showed better activity to the biofilm which has been formed or is being formed. In addition to this, the obvious interaction between bacteria/biofilm and LA-Bac8c was observed by microscopy. LA-Bac8c displayed strong membrane depolarization and outer membrane permeabilizing ability, and the cell membrane treated with LA-Bac8c was destroyed to the leakage of bacteria cellular components. All these data indicated LA-Bac8c could be used as a useful antimicrobial peptide with wide application prospect.