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Bactericidal and anti-biofilm activity of ebastine against Staphylococcus aureus.

Liping Zhao1, Hui Zhang1, Li Zha1

  • 1The Second Affiliated Hospital of Jiaxing University, Jiaxing 314000 Zhejiang, China.

Letters in Applied Microbiology
|June 12, 2025
PubMed
Summary

The antihistamine drug ebastine shows potent bactericidal and anti-biofilm activity against drug-resistant Staphylococcus aureus. Ebastine disrupts bacterial membranes and generates reactive oxygen species, offering a promising new antimicrobial therapy.

Keywords:
MRSAanti-biofilmbactericidaldrug repurposingebastine

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Area of Science:

  • Microbiology
  • Pharmacology
  • Drug Discovery

Background:

  • Multidrug-resistant bacteria pose a significant threat to public health.
  • Drug repurposing is a viable strategy to discover novel antimicrobial agents.
  • Staphylococcus aureus is a major cause of bacterial infections, often exhibiting resistance to antibiotics.

Purpose of the Study:

  • To investigate the antimicrobial potential of the antihistamine drug ebastine against Staphylococcus aureus.
  • To evaluate ebastine's bactericidal activity, anti-biofilm properties, and mechanisms of action.
  • To assess the safety profile of ebastine for potential therapeutic use.

Main Methods:

  • Minimum Inhibitory Concentrations (MICs) were determined using broth microdilution.
  • Time-kill curve analyses assessed bactericidal kinetics.
  • Biofilm inhibition and eradication assays were performed.
  • Mechanistic studies involved bacterial membrane integrity and reactive oxygen species (ROS) generation assays.
  • Mammalian cell toxicity and hemolytic assays evaluated safety.

Main Results:

  • Ebastine demonstrated significant activity against S. aureus isolates, with MIC values ranging from 2 to 8 µg·mL-1.
  • A dose-dependent bactericidal effect was observed.
  • Ebastine inhibited biofilm formation and moderately eradicated preformed biofilms.
  • Mechanisms involved bacterial membrane disruption and ROS generation.
  • Ebastine showed limited toxicity to mammalian cells with negligible hemolytic effects.

Conclusions:

  • Ebastine possesses significant bactericidal and anti-biofilm properties against Staphylococcus aureus.
  • The drug's mechanism involves membrane damage and ROS induction.
  • Ebastine exhibits a favorable safety profile, suggesting its potential as a novel antimicrobial agent for drug-resistant infections.