Halogenated boroxine dipotassium trioxohydroxytetrafluorotriborate K2[B3O3F4OH] inhibits emerging multidrug-resistant and β-lactamase-producing opportunistic pathogens

Drug Dev Ind Pharm. 2019 Nov;45(11):1770-1776. doi: 10.1080/03639045.2019.1656736. Epub 2019 Sep 2.

Abstract

Halogenated boroxine dipotassium trioxohydroxytetrafluorotriborate, K2[B3O3F4OH] (boroxine) was previously shown to be very effective in inhibition of several carcinoma cell lines, including the skin cancer. Here, we investigated its antimicrobial potential by targeting the multidrug-resistant opportunistic pathogens associated with skin and wound infections. The antimicrobial testing against eleven bacterial and four fungal species revealed good activity of boroxine against pathogenic filamentous fungi Penicillium funiculosum and Aspergillus niger (MIC50 64 and 128 µg/ml), and a moderate bioactivity against the yeast Candida albicans (MIC50 512 µg/ml). Among the tested multidrug-resistant bacteria, the best antibacterial effect, stable over a 24-h period, was observed against the methicillin-resistant Staphylococcus aureus strain (MRSA) at MIC of 1024 µg/ml. The atomic force microscopy (AFM) used to investigate the morphology of S. aureus cells revealed indentations on its cell envelope after the boroxine exposure. These results show that in addition to the antitumor effect, boroxine exerts wide spectrum antimicrobial activity, thus may help preventing the development of skin and wound-related opportunistic infections.

Keywords: Atomic force microscopy; MRSA; boroxine; membrane permeability; multidrug-resistant pathogens.

MeSH terms

  • Aspergillus niger / drug effects
  • Aspergillus niger / metabolism
  • Boron Compounds / chemistry
  • Boron Compounds / pharmacology*
  • Boron Compounds / therapeutic use
  • Candida albicans / drug effects
  • Candida albicans / metabolism
  • Drug Resistance, Multiple, Bacterial / drug effects*
  • Halogenation
  • Humans
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Methicillin-Resistant Staphylococcus aureus / metabolism
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Opportunistic Infections / microbiology
  • Opportunistic Infections / prevention & control*
  • Penicillium / drug effects
  • Penicillium / metabolism
  • Skin Diseases, Infectious / microbiology
  • Skin Diseases, Infectious / prevention & control
  • Wound Infection / microbiology
  • Wound Infection / prevention & control
  • beta-Lactam Resistance / drug effects*
  • beta-Lactamase Inhibitors / chemistry
  • beta-Lactamase Inhibitors / pharmacology*
  • beta-Lactamase Inhibitors / therapeutic use
  • beta-Lactamases / metabolism

Substances

  • Boron Compounds
  • beta-Lactamase Inhibitors
  • dipotassium trioxohydroxytetrafluorotriborate
  • beta-Lactamases