2. Academic Validation
  3. Lipoic acid modified antimicrobial peptide with enhanced antimicrobial properties

Lipoic acid modified antimicrobial peptide with enhanced antimicrobial properties

  • Bioorg Med Chem. 2020 Oct 1;28(19):115682. doi: 10.1016/j.bmc.2020.115682.
Wenya Zhou 1,  Yawei Du 1,  Xinsong Li 1,  Chen Yao 2
Affiliations

Affiliations

  • 1 School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, PR China.
  • 2 School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, PR China. Electronic address: cyao@seu.edu.cn.
PMID: 32912428 DOI: 10.1016/j.bmc.2020.115682
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.

Keywords

Antibiofilm activity; Antimicrobial peptide; Bac8c; Lipoic acid; Membrane depolarization; Membrane permeability.

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