ArticleArchives of microbiology2025
Antibacterial and anti-biofilm activities of Derazantinib (ARQ-087) against Staphylococcus aureus.
Article in Archives of microbiology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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3 authors.
Funding
Abstract
The global rise of multidrug-resistant pathogens, particularly methicillin-resistant Staphylococcus aureus (MRSA), represents a critical public health challenge. This study evaluates the antibacterial and anti-biofilm activities of Derazantinib (ARQ-087) against S. aureus. ARQ-087 exhibited minimum inhibitory concentration (MIC) values ranging from 4 to 16 µM against S. aureus reference laboratory strains and diverse clinical MRSA isolates, demonstrating strong antibacterial activity with minimal resistance development. Time-kill assays demonstrated a concentration- and time-dependent reduction in bacterial viability. Crystal violet staining assays revealed that ARQ-087 significantly inhibited MRSA biofilm formation in a dose-dependent manner. Additionally, ARQ-087 exhibited strong anti-biofilm activity against pre-formed biofilms, as shown by colony counts and confocal laser scanning microscopy, which indicated extensive biofilm disruption and bacterial cell death. Mechanistic studies revealed that ARQ-087 disrupts bacterial membrane integrity, as evidenced by SYTOX Green and DISC3(5) fluorescence assays, while inducing intracellular ATP depletion and reactive oxygen species generation, contributing to bacterial death. ARQ-087 also displayed negligible hemolytic activity and no acute toxicity observed in a Galleria mellonella infection model. In this model, ARQ-087 prolonged the survival of larvae infected with S. aureus. These findings highlight ARQ-087 as a promising therapeutic candidate for treating MRSA infections and biofilm-associated diseases. Further preclinical studies are needed to confirm its potential for clinical application.
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