doi:10.1186/s12866-024-03377-3...
BioMed Central
Mycology
2024
03/07/2024
Multi-drug-resistant Staphylococcus aureus infections necessitate novel antibiotic development.
D-3263, a transient receptor potential melastatin member 8 (TRPM8) agonist, has potential antineoplastic properties.
Here, we reported the antibacterial and antibiofilm activities of D-3263.
Minimum inhibitory concentrations (MICs) against S. aureus , Enterococcus faecalis and E. faecium were ≤ 50 µM.
D-3263 exhibited bactericidal effects against clinical methicillin-resistant S. aureus (MRSA) and E. faecalis strains at 4× MIC.
Subinhibitory D-3263 concentrations effectively inhibited S. aureus and E. faecalis biofilms, with higher concentrations also clearing mature biofilms.
Proteomic analysis revealed differential expression of 29 proteins under 1/2 × MIC D-3263, influencing amino acid biosynthesis and carbohydrate metabolism.
Additionally, D-3263 enhanced membrane permeability of S. aureus and E. faecalis .
Bacterial membrane phospholipids phosphatidylethanolamine (PE), phosphatidylglycerol (PG), and cardiolipin (CL) dose-dependently increased D-3263 MICs.
Overall, our data suggested that D-3263 exhibited potent antibacterial and antibiofilm activities against S. aureus by targeting the cell membrane.
Liu, Xiaoju,Xiong, Yanpeng,Peng, Renhai,Zhang, Yufang,Cai, Shuyu,Deng, Qiwen,Yu, Zhijian,Wen, Zewen,Chen, Zhong,Hou, Tieying, 2024, Antibacterial activity and mechanisms of D-3263 against Staphylococcus aureus, BioMed Central