Antibacterial activity and mechanisms of D-3263 against Staphylococcus aureus.
BMC Microbiol
; 24(1): 224, 2024 Jun 26.
Article
in En
| MEDLINE
| ID: mdl-38926818
ABSTRACT
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Staphylococcus aureus
/
Microbial Sensitivity Tests
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Enterococcus faecalis
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Biofilms
/
Anti-Bacterial Agents
Limits:
Humans
Language:
En
Journal:
BMC Microbiol
/
BMC microbiol
/
BMC microbiology
Journal subject:
MICROBIOLOGIA
Year:
2024
Type:
Article
Affiliation country:
China