Carbonyl cyanide -nitrophenylhydrazone (2e) displayed a lone or synergistic efficacy against MRSA (, 2020, 10, 17854). In this work, the synergistic mechanism of 2e with ofloxacin was studied. MRSA2858 had potential for biofilm formation, and the value of MBEC of 2e alone was 0.78-1.56 μM, while that of 2e + ofloxacin was 0.39-0.78 μM. 2e combined with ofloxacin showed a synergistic anti-biofilm effect against MRSA. Efflux pump inhibitor 2e can better bind to NorA protein. After MRSA2858 was treated with 2e of 1/2MIC (0.78 μM) and ofloxacin of 1/8MIC (0.097 μM), the transcript levels of efflux genes () and quorum-sensing (QS) regulatory genes (, , , ) were substantially down-regulated, and alpha-hemolysin (Hla) was inhibited by 99.15%. 2e combined with ofloxacin was more effective than 2e alone in reducing bacterial load . All in all, efflux pump inhibitor 2e enhanced the bactericidal activities of antibiotics through regulating the gene expression of NorA and QS system.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9850365 | PMC |
| http://dx.doi.org/10.1039/d2ra06696c | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Specificity and tunability of efflux pumps: A new role for the proton gradient?
PLoS Comput Biol
January 2025
Department of Physics, University of Toronto, Toronto, Ontario, Canada.
Efflux pumps that transport antibacterial drugs out of bacterial cells have broad specificity, commonly leading to broad spectrum resistance and limiting treatment strategies for infections. It remains unclear how efflux pumps can maintain this broad spectrum specificity to diverse drug molecules while limiting the efflux of other cytoplasmic content. We have investigated the origins of this broad specificity using theoretical models informed by the experimentally determined structural and kinetic properties of efflux pumps.
View Article and Find Full Text PDFTemporal dynamics of the soil resistome and microbiome irrigated with treated wastewater containing clarithromycin.
Environ Res
January 2025
INRAE, University of Montpellier, LBE, Av. des Étangs, 11100 Narbonne, France.
Clarithromycin, a common antibiotic found in domestic wastewater, persists even after treatment and can transfer to soils when treated wastewater (TWW) is used for irrigation. This residual antibiotic may exert selection pressure, promoting the spread of antibiotic resistance. While Predicted No Effect Concentrations (PNECs) are used in liquid media to predict resistance risks, PNEC values for soils, especially for clarithromycin, are lacking.
View Article and Find Full Text PDFTargeting Acinetobacter baumannii resistance-nodulation-division efflux pump transcriptional regulators to combat antimicrobial resistance.
NPJ Antimicrob Resist
January 2025
Department of Microbiology, University of Manitoba, Winnipeg, MB, Canada.
Regulatory elements controlling gene expression fine-tune bacterial responses to environmental cues, including antimicrobials, to optimize survival. Acinetobacter baumannii, a pathogen notorious for antimicrobial resistance, relies on efficient efflux systems. Though the role of efflux systems in antibiotic expulsion are well recognized, the regulatory mechanisms controlling their expression remain understudied.
View Article and Find Full Text PDFPharmacological, computational, and mechanistic insights into triptolide's role in targeting drug-resistant cancers.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Research and Enterprise, University of Cyberjaya, Persiaran Bestari, Cyber 11, 63000, Cyberjaya, Selangor, Malaysia.
As a promising candidate for tackling drug-resistant cancers, triptolide, a diterpenoid derived from the Chinese medicinal plant Tripterygium wilfordii, has been developed. This review summarizes potential antitumor activities, including the suppression of RNA polymerase II, the suppression of heat shock proteins (HSP70 and HSP90), and the blockade of NF-kB signalling. Triptolide is the first known compound to target cancer cells specifically but spare normal cells, and it has success in treating cancers that are difficult to treat, including pancreatic, breast, and lung cancers.
View Article and Find Full Text PDFAntibacterial Potential of Crude Extracts from NR125682 and NR117881.
Microorganisms
January 2025
Department of Biochemistry and Microbiology, University of Zululand, Richards Bay 3886, South Africa.
The challenges of antimicrobial resistance (AMR) to human health have pushed for the discovery of a new antibiotics agent from natural products. Cyanobacteria are oxygen-producing photosynthetic prokaryotes found in a variety of water habitats. Secondary metabolites are produced by cyanobacteria to survive extreme environmental stress factors, including microbial competition.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!