Uncovering nitroxoline activity spectrum, mode of action and resistance across Gram-negative bacteria

Abstract Nitroxoline is a bacteriostatic quinoline antibiotic, known to form complexes with metals. Its clinical indications are limited to uncomplicated urinary tract infections, with a susceptibility breakpoint only available for Escherichia coli. Here, we test > 1000 clinical isolates and demo...

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Main Authors: Elisabetta Cacace, Manuela Tietgen, Meike Steinhauer, André Mateus, Tilman G. Schultze, Marina Eckermann, Marco Galardini, Vallo Varik, Alexandra Koumoutsi, Jordan J. Parzeller, Federico Corona, Askarbek Orakov, Michael Knopp, Amber Brauer-Nikonow, Peer Bork, Celia V. Romao, Michael Zimmermann, Peter Cloetens, Mikhail M. Savitski, Athanasios Typas, Stephan Göttig
Format: Article
Language:English
Published: Nature Portfolio 2025-04-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-025-58730-5
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Summary:Abstract Nitroxoline is a bacteriostatic quinoline antibiotic, known to form complexes with metals. Its clinical indications are limited to uncomplicated urinary tract infections, with a susceptibility breakpoint only available for Escherichia coli. Here, we test > 1000 clinical isolates and demonstrate a much broader activity spectrum and species-specific bactericidal activity, including Gram-negative bacteria for which therapeutic options are limited due to multidrug resistance. By combining genetic and proteomic approaches with direct measurement of intracellular metals, we show that nitroxoline acts as a metallophore, inducing copper and zinc intoxication in bacterial cells. The compound displays additional effects on bacterial physiology, including alteration of outer membrane integrity, which underpins nitroxoline’s synergies with large-scaffold antibiotics and resensitization of colistin-resistant Enterobacteriaceae in vitro and in vivo. Furthermore, we identify conserved resistance mechanisms across bacterial species, often leading to nitroxoline efflux.
ISSN:2041-1723