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© Research
Publication : Future microbiology

1-benzyl-1,4-diazepane reduces the efflux of resistance-nodulation-cell division pumps in Escherichia coli.

Team: Parasite RNA Biology
Member: Tiziano Vignolini
Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Future microbiology - 01 Jul 2020

Casalone E, Vignolini T, Braconi L, Gardini L, Capitanio M, Pavone FS, Dei S, Teodori E

Link to Pubmed [PMID] – 32840130

Link to DOI – 10.2217/fmb-2019-0296

Future Microbiol 2020 Jul; 15(): 987-999

Aim: To investigate the action mechanism of 1-benzyl-1,4-diazepane (1-BD) as efflux pump inhibitor (EPI) in Escherichia coli mutants: ΔacrAB or overexpressing AcrAB and AcrEF efflux pumps. Materials & methods: Effect of 1-BD on: antibiotic potentiation, by microdilution method; membrane functionality, by fluorimetric assays; ethidium bromide accumulation, by fluorometric real-time efflux assay; AcrB expression, by quantitative photoactivated localization microscopy. Results: 1-BD decreases the minimal inhibitory concentration of levofloxacin and other antibiotics and increase ethidium bromide accumulation in E. coli overexpressing efflux pumps but not in the ΔacrAB strain. 1-BD increases membranes permeability, without sensibly affecting inner membrane polarity and decreases acrAB transcription. Conclusion: 1-BD acts as an EPI in E. coli with a mixed mechanism, different from that of major reference EPIs.