Phytomedicine, Journal Year: 2025, Volume and Issue: 143, P. 156821 - 156821
Published: May 1, 2025
Language: Английский
Phytomedicine, Journal Year: 2025, Volume and Issue: 143, P. 156821 - 156821
Published: May 1, 2025
Language: Английский
Published: Jan. 1, 2025
Language: Английский
Citations
0Antibiotics, Journal Year: 2025, Volume and Issue: 14(3), P. 231 - 231
Published: Feb. 25, 2025
Background/Objectives: Streptococcus pneumoniae (S. pneumoniae) is a major pathogen causing severe infectious diseases, with an escalating issue of antimicrobial resistance that threatens the efficacy existing antibiotics. Given challenges in developing traditional antibiotics, drug repurposing strategies offer novel approach to address crisis. This study aims evaluate antibacterial and anti-biofilm activities approved non-antibiotic anticancer carmofur against multidrug-resistant S. pneumoniae, investigate mechanism action, assess therapeutic potential vivo. Methods/Results: Antimicrobial tests revealed exhibited strong activity strains, minimum inhibitory concentrations (MICs) ranging from 0.25 1 µg/mL. In biofilm detection experiments, not only inhibited formation biofilms, but also effectively removed biofilms under high concentration conditions. Mechanistic studies showed disrupted bacterial membrane permeability decreased intracellular ATP levels. Molecular docking dynamics simulation assays indicated could stably bind thymidylate synthase through hydrogen bonding hydrophobic interactions, thereby exerting effects. Meanwhile, was able repress expression thyA gene at mRNA level. mouse infection model, treatment group reduction approximately two log levels load lung tissue blood, significant decrease inflammatory cytokines TNF-α IL-6, improvement survival rate 60%. Conclusions: summary, demonstrated good anti-infective effects vivo, suggesting its clinical application as agent drug-resistant bacteria.
Language: Английский
Citations
0Frontiers in Microbiology, Journal Year: 2025, Volume and Issue: 16
Published: March 20, 2025
Background Methicillin-resistant Staphylococcus aureus (MRSA) poses a significant clinical challenge due to its multidrug resistance. Diacerein (DIA), primarily used treat degenerative joint diseases, has recently been found exhibit antibacterial activity, though specific mechanisms remain unclear. Methods The minimum inhibitory concentration (MIC) and bactericidal (MBC) of DIA, as well in - vitro combination susceptibility testing, were determined using the broth microdilution method. Additionally, resistance induction assays, time-growth curve measurements, membrane fluidity, intracellular protein levels, reactive oxygen species (ROS) assessed. inhibition clearance MRSA biofilms by DIA evaluated crystal violet staining method, with bacterial morphology observed via scanning electron microscopy confocal laser microscopy. Finally, transcriptome analysis was conducted identify gene expression changes treated RT-qPCR verification performed. Results MIC MBC against 32 μg/mL 128 μg/mL, respectively, synergistic effects when combined ampicillin. increased ROS levels fluidity MRSA, decreased soluble synthesis, altered morphology. significantly inhibited biofilm formation disrupted pre existing biofilms. Transcriptome revealed 1,045 differentially expressed genes between DIA-treated group control group, involving pathways such tricarboxylic acid cycle, phosphorylation, ribosome metabolism, nucleotide metabolism. Conclusion In summary, anti-biofilm activities does not easily induce Its may involve multiple aspects, including energy
Language: Английский
Citations
0Phytomedicine, Journal Year: 2025, Volume and Issue: 143, P. 156821 - 156821
Published: May 1, 2025
Language: Английский
Citations
0