Antimicrobial activity of nitrochalcone and pentyl caffeate against hospital pathogens results in decreased microbial adhesion and biofilm formation

Biofouling. 2019 Feb;35(2):129-142. doi: 10.1080/08927014.2019.1574763. Epub 2019 Apr 5.

Abstract

The present study investigated the antimicrobial, anti-adhesion and anti-biofilm activity of the modified synthetic molecules nitrochalcone (NC-E05) and pentyl caffeate (C5) against microorganisms which have a high incidence in hospital-acquired infections. The compounds were further tested for their preliminary systemic toxicity in vivo. NC-E05 and C5 showed antimicrobial activity, with minimum inhibitory concentrations (MICs) ranging between 15.62 and 31.25 μg ml-1. Treatment with NC-E05 and C5 at 1 × MIC and/or 10 × MIC significantly reduced mono or mixed-species biofilm formation and viability. At MIC/2, the compounds decreased microbial adhesion to HaCaT keratinocytes from 1 to 3 h (p < 0.0001). In addition, NC-E05 and C5 demonstrated low toxicity in vivo in the Galleria mellonella model at anti-biofilm concentrations. Thus, the chemical modification of these molecules proved to be effective in the proposed anti-biofilm activity, opening opportunities for the development of new antimicrobials.

Keywords: Mixed biofilm; nitrochalcone; pentyl caffeate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / toxicity
  • Anti-Infective Agents / pharmacology*
  • Anti-Infective Agents / toxicity
  • Antifungal Agents / pharmacology
  • Antifungal Agents / toxicity
  • Bacterial Adhesion / drug effects*
  • Biofilms / drug effects*
  • Biofilms / growth & development
  • Caffeic Acids / pharmacology*
  • Caffeic Acids / toxicity
  • Candida albicans / drug effects
  • Cell Line
  • Cell Survival / drug effects
  • Chalcones / pharmacology*
  • Chalcones / toxicity
  • Cross Infection / prevention & control
  • Humans
  • Keratinocytes / cytology
  • Keratinocytes / drug effects
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Microbial Sensitivity Tests
  • Moths / drug effects
  • Staphylococcus aureus / drug effects

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Antifungal Agents
  • Caffeic Acids
  • Chalcones