Rapid High-Throughput Assay Identified Gemcitabine and Derivatives As Potent Inhibitors Against Multidrug-Resistant Staphylococcus aureus .
Zhao ChenJinxiu LiYue WanRuisong BaiWenjuan WangXuan GaoDi LiQingfeng HuYong LiBenfang Helen RuanPublished in: Assay and drug development technologies (2022)
Methicillin-resistant Staphylococcus aureus (MRSA) are challenging pathogenic bacteria that can cause severe infection leading to high mortality rates. We found that both the oxacillin- and cefoxitin-resistant S. aureus strains isolated from clinic showed multidrug-resistant (MDR) characteristics. Through rapid high-throughput screen (HTS) of a compound library, gemcitabine and selen compounds were found to effectively inhibit S. aureus growth. For further improvement, we synthesized selen-containing gemcitabine that demonstrated relatively potent antimicrobial activity against several MDR MRSA in vitro . The HTS assay and gemcitabine selen derivative provided a useful tool to explore an effective molecular target to treat MDR MRSA.
Keyphrases
- methicillin resistant staphylococcus aureus
- multidrug resistant
- high throughput
- staphylococcus aureus
- drug resistant
- gram negative
- acinetobacter baumannii
- locally advanced
- klebsiella pneumoniae
- single cell
- biofilm formation
- escherichia coli
- squamous cell carcinoma
- anti inflammatory
- rectal cancer
- loop mediated isothermal amplification
- type diabetes
- risk factors
- cardiovascular events
- early onset
- pseudomonas aeruginosa
- cystic fibrosis
- water soluble
- sensitive detection