Antimicrobial and anti-biofilm activity of a thiazolidinone derivative against Staphylococcus aureus in vitro and in vivo
Methicillin-Resistant Staphylococcus aureus
570
Staphylococcus aureus
610
WalK
Microbial Sensitivity Tests
Staphylococcal Infections
bacteriocidal
Microbiology
QR1-502
Anti-Bacterial Agents
Mice
anti-biofilm activity
Biofilms
Chlorocebus aethiops
Humans
Animals
Vero Cells
Research Article
DOI:
10.1128/spectrum.02327-23
Publication Date:
2024-02-08T14:01:26Z
AUTHORS (9)
ABSTRACT
ABSTRACT
Staphylococcus aureus
(
S. aureus
) causes many infections with significant morbidity and mortality.
S. aureus
can form biofilms, which can cause biofilm-associated diseases and increase resistance to many conventional antibiotics, resulting in chronic infection. It is critical to develop novel antibiotics against staphylococcal infections, particularly those that can kill cells embedded in biofilms. This study aimed to investigate the bacteriocidal and anti-biofilm activities of thiazolidinone derivative (TD-H2-A) against
S. aureus
. A total of 40 non-duplicate strains were collected, and the minimum inhibitory concentrations (MICs) of TD-H2-A were determined. The effect of TD-H2-A on established
S. aureus
mature biofilms was examined using a confocal laser scanning microscope (CLSM). The antibacterial effects of the compound on planktonic bacteria and bacteria in mature biofilms were investigated. Other characteristics, such as cytotoxicity and hemolytic activity, were researched. A mouse skin infection model was used, and a routine hematoxylin and eosin (H&E) staining was used for histological examination. The MIC values of TD-H2-A against the different
S. aureus
strains were 6.3–25.0 µg/mL. The 5 × MIC TD-H2-A killed almost all planktonic
S. aureus
USA300. The derivative was found to have strong bacteriocidal activity against cells in mature biofilms meanwhile having low cytotoxicity and hemolytic activity against Vero cells and human erythrocytes. TD-H2-A had a good bacteriocidal effect on
S. aureus
SA113-infected mice. In conclusion, TD-H2-A demonstrated good bacteriocidal and anti-biofilm activities against
S. aureus
, paving the way for the development of novel agents to combat biofilm infections and multidrug-resistant staphylococcal infections.
IMPORTANCE
Staphylococcus aureus
, a notorious pathogen, can form a stubborn biofilm and develop drug resistance. It is crucial to develop new anti-infective therapies against biofilm-associated infections. The manuscript describes the new antibiotic to effectively combat multidrug-resistant and biofilm-associated diseases.
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