Antimicrobial action of the cyclic peptide bactenecin on Burkholderia pseudomallei correlates with efficient membrane permeabilization

PLoS Negl Trop Dis. 2013 Jun 13;7(6):e2267. doi: 10.1371/journal.pntd.0002267. Print 2013.

Abstract

Burkholderia pseudomallei is a category B agent that causes Melioidosis, an acute and chronic disease with septicemia. The current treatment regimen is a heavy dose of antibiotics such as ceftazidime (CAZ); however, the risk of a relapse is possible. Peptide antibiotics are an alternative to classical antibiotics as they exhibit rapid action and are less likely to result in the development of resistance. The aim of this study was to determine the bactericidal activity against B. pseudomallei and examine the membrane disrupting abilities of the potent antimicrobial peptides: bactenecin, RTA3, BMAP-18 and CA-MA. All peptides exhibited >97% bactericidal activity at 20 µM, with bactenecin having slightly higher activity. Long term time-kill assays revealed a complete inhibition of cell growth at 50 µM bactenecin and CA-MA. All peptides inhibited biofilm formation comparable to CAZ, but exhibited faster kinetics (within 1 h). Bactenecin exhibited stronger binding to LPS and induced perturbation of the inner membrane of live cells. Interaction of bactenecin with model membranes resulted in changes in membrane fluidity and permeability, leading to leakage of dye across the membrane at levels two-fold greater than that of other peptides. Modeling of peptide binding on the membrane showed stable and deep insertion of bactenecin into the membrane (up to 9 Å). We propose that bactenecin is able to form dimers or large β-sheet structures in a concentration dependent manner and subsequently rapidly permeabilize the membrane, leading to cytosolic leakage and cell death in a shorter period of time compared to CAZ. Bactenecin might be considered as a potent antimicrobial agent for use against B. pseudomallei.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Burkholderia pseudomallei / drug effects*
  • Burkholderia pseudomallei / physiology
  • Cell Membrane / drug effects*
  • Cell Membrane / physiology
  • Cell Membrane Permeability / drug effects*
  • Microbial Viability / drug effects
  • Peptides, Cyclic / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Peptides, Cyclic
  • bactenecin

Grants and funding

Research grant support of this study was from co-funding between Thailand Research Fund, Office of the Higher Education Commission and Khon Kaen University under grant number MRG5280019 and under supervision of S. Daduang. The simulation work of A. L. Lomize was supported by the Division of Biological Infrastructure of the National Science Foundation (award # 1145367). Part of this work was supported by the Higher Education Research Promotion and National Research University Project of Thailand, Office of the Higher Education Commission, through the Food and Functional Food Research Cluster of Khon Kaen University. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.