Evaluation of antibacterial and antibiofilm mechanisms by usnic acid against methicillin-resistant Staphylococcus aureus

Future Microbiol. 2016 Oct:11:1315-1338. doi: 10.2217/fmb-2016-0049. Epub 2016 Sep 16.

Abstract

Aim: To evaluate the antibacterial and antibiofilm mechanisms of usnic acid (USN) against methicillin-resistant Staphylococcus aureus from cystic fibrosis patients.

Materials & methods: The effects exerted by USN at subinhibitory concentrations on S. aureus Sa3 strain was evaluated by proteomic, real-time PCR and electron microscopy analyses.

Results & conclusion: Proteomic analysis showed that USN caused damage in peptidoglycan synthesis, as confirmed by microscopy. Real-time PCR analysis showed that antibiofilm activity of USN is mainly due to impaired adhesion to the host matrix binding proteins, and decreasing lipase and thermonuclease expression. Our data show that USN exerts anti-staphylococcal effects through multitarget inhibitory effects, thus confirming the rationale for considering it 'lead compound' for the treatment of cystic fibrosis infections.

Keywords: Staphylococcus aureus; biofilm; usnic acid.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adhesins, Bacterial / drug effects
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / pharmacology*
  • Bacterial Proteins / antagonists & inhibitors
  • Bacterial Proteins / drug effects
  • Bacterial Proteins / genetics
  • Bacterial Proteins / metabolism
  • Benzofurans / administration & dosage
  • Benzofurans / pharmacology*
  • Biofilms / drug effects*
  • Carrier Proteins / drug effects
  • Cell Membrane / drug effects
  • Cell Survival / drug effects
  • Colony Count, Microbial
  • Cystic Fibrosis / drug therapy
  • Cystic Fibrosis / microbiology
  • DNA, Bacterial
  • Down-Regulation
  • Lipase / drug effects
  • Methicillin-Resistant Staphylococcus aureus / drug effects*
  • Methicillin-Resistant Staphylococcus aureus / genetics
  • Methicillin-Resistant Staphylococcus aureus / pathogenicity
  • Methicillin-Resistant Staphylococcus aureus / ultrastructure
  • Microbial Sensitivity Tests
  • Microbial Viability / drug effects
  • Microscopy, Electron, Scanning / methods
  • Microscopy, Electron, Transmission / methods
  • Peptidoglycan / biosynthesis
  • Peptidoglycan / drug effects
  • Propidium / metabolism
  • Protein Interaction Maps
  • Proteomics / methods
  • Real-Time Polymerase Chain Reaction / methods
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization / methods
  • Staphylococcal Infections / microbiology
  • Time Factors
  • Virulence / drug effects
  • Virulence / genetics

Substances

  • Adhesins, Bacterial
  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Benzofurans
  • Carrier Proteins
  • DNA, Bacterial
  • Peptidoglycan
  • usnic acid
  • Propidium
  • Lipase