Synergy Between the Auranofin Analogue PEt3AuCl and Membrane Disruptors, Efflux-Pump Blockers, and Glutathione-Depletors Uncovers Tolerance Pathways in Pseudomonas aeruginosa

Auranofin (AF), an FDA-approved drug for rheumatoid arthritis, exhibits strong antibacterial activity against Gram-positive bacteria, while Gram-negative species remain largely tolerant. This study assessed the antimicrobial activity of AF and three analogues against clinically relevant Gram-negative pathogens and explored tolerance mechanisms in Pseudomonas aeruginosa. Broth microdilution assays were performed on reference strains and clinical isolates of Escherichia coli, Klebsiella pneumoniae, and P. aeruginosa. Synergy studies with the most active analogue, PEt3AuCl (AF-Cl), were conducted against P. aeruginosa using polymyxin B (PMB), two efflux-pump inhibitors, and two glutathione (GSH) depletors. Gold compounds showed MICs between 4 and >64 µg/mL, with AF-Cl displaying the highest activity. AF-Cl activity was markedly enhanced by PMB and efflux-pump inhibitors, indicating that outer membrane permeability and efflux contribute to tolerance. Additionally, GSH depletion significantly potentiated AF-Cl, implicating redox homeostasis in resistance. Overall, AF-Cl shows potential against Gram-negative bacteria when combined with agents targeting membrane integrity, efflux systems, or redox balance, supporting combinatorial strategies to overcome resistance in P. aeruginosa and related pathogens.

Authors

Institutions

Publication Details

Journal
International Journal of Molecular Sciences
Published
2026-05-21
DOI
https://doi.org/10.3390/ijms27104610
Primary Topic
Redox biology and oxidative stress
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Synergy Between the Auranofin Analogue PEt3AuCl and Membrane Disruptors, Efflux-Pump Blockers, and Glutathione-Depletors Uncovers Tolerance Pathways in Pseudomonas aeruginosa

Semih Esin, Diletta Mazzantini, Giuseppantonio Maisetta, Giovanna Batoni et al.
International Journal of Molecular Sciences
Redox biology and oxidative stress
article

Synergy Between the Auranofin Analogue PEt3AuCl and Membrane Disruptors, Efflux-Pump Blockers, and Glutathione-Depletors Uncovers Tolerance Pathways in Pseudomonas aeruginosa

Semih Esin, Diletta Mazzantini, Giuseppantonio Maisetta, Giovanna Batoni, José Aleixo de Azevedo-França, Luigi Messori, Emilia Ghelardi, Beatrice Amato
article en

Abstract

Auranofin (AF), an FDA-approved drug for rheumatoid arthritis, exhibits strong antibacterial activity against Gram-positive bacteria, while Gram-negative species remain largely tolerant. This study assessed the antimicrobial activity of AF and three analogues against clinically relevant Gram-negative pathogens and explored tolerance mechanisms in Pseudomonas aeruginosa. Broth microdilution assays were performed on reference strains and clinical isolates of Escherichia coli, Klebsiella pneumoniae, and P. aeruginosa. Synergy studies with the most active analogue, PEt3AuCl (AF-Cl), were conducted against P. aeruginosa using polymyxin B (PMB), two efflux-pump inhibitors, and two glutathione (GSH) depletors. Gold compounds showed MICs between 4 and >64 µg/mL, with AF-Cl displaying the highest activity. AF-Cl activity was markedly enhanced by PMB and efflux-pump inhibitors, indicating that outer membrane permeability and efflux contribute to tolerance. Additionally, GSH depletion significantly potentiated AF-Cl, implicating redox homeostasis in resistance. Overall, AF-Cl shows potential against Gram-negative bacteria when combined with agents targeting membrane integrity, efflux systems, or redox balance, supporting combinatorial strategies to overcome resistance in P. aeruginosa and related pathogens.

International Journal of Molecular SciencesVol. 27(10)
University of Pisa (IT), University of Florence (IT)
Openalex Percentile: Top 9%
Redox biology and oxidative stress
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.