Antibacterial Activity of Squaric Amide Derivative SA2 against Methicillin-Resistant Staphylococcus aureus
Abstract
:1. Introduction
2. Results
2.1. Chemistry
2.2. Screening and Validation of the SA Derivate with Potent Activity against MRSA
2.3. Inhibitory Activity of SA2 to the Growth Curves and the Colony Formation Unit of MRSA
2.4. Effect of SA2 on the Morphologies of MRSA
2.5. Therapeutic Efficacy of SA2 on MRSA-Induced Skin Infection
2.6. SA2 Disrupted Alanine Dehydrogenase-Dependent NAD+/NADH Homeostasis
3. Discussion
4. Materials and Methods
4.1. Bacterial Strains, Cells, and Chemicals
4.2. Synthesis and Characterization of SAs
4.3. Determination of Minimal Inhibitory Concentration (MIC)
4.4. Bacterial Growth Curve Assay
4.5. Time-Kill Assay
4.6. MRSA-Induced Skin Infection Animal Model
4.7. Electron Microscopy Observation
4.8. Transcriptome Analysis
4.9. Real-Time PCR
4.10. Statistical Analysis
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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Microorganism | MIC (µg/mL) |
---|---|
Staphylococcus aureus (MSSA, ATCC 29213) | 2–4 |
Staphylococcus aureus (MSSA, ATCC43300) | 4 |
Staphylococcus aureus (MRSA, VISA, Mu50) | 4 |
Staphylococcus aureus (MRSA, USA300) | 4 |
Staphylococcus aureus (MRSA, clinical strain XJ 26) | 8 |
Staphylococcus aureus (MRSA, clinical strain XJ 216) | 8 |
Staphylococcus aureus (MRSA, clinical strain XJ 317) | 8 |
Staphylococcus aureus (MRSA, clinical strain XJ 141240) | 8 |
Staphylococcus epidermidis (ATCC14990) | 8 |
Staphylococcus epidermidis (MRSE, clinical strain XJ 537) | 4 |
Enterococcus faecalis (ATCC29212) | 4 |
Enterococcus faecalis (VER clinical strain XJ 21) | 8 |
Enterococcus faecalis (VER clinical strain XJ 22) | 8 |
Enterococcus faecalis (VER clinical strain XJ 23) | 8 |
Escherichia coli (ATCC 25922) | >256 |
Escherichia coli (MDR, clinical strain XJ 74283) | >256 |
Salmonella typhimurium (MDR, SL1344) | >256 |
Acinetobacter baumannii (ATCC 19606) | >256 |
Pseudomonas aeruginosa (ATCC 27853) | >256 |
Pseudomonas aeruginosa (MDR, clinical strain XJ 75315) | >256 |
Klebsiella pneumoniae (ATCC700603) | >256 |
Klebsiella pneumoniae (ATCC13885) | >256 |
Klebsiella pneumoniae (MDR, ATCC 75297) | >256 |
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Yu, M.; Hou, Y.; Cheng, M.; Liu, Y.; Ling, C.; Zhai, D.; Zhao, H.; Li, Y.; Chen, Y.; Xue, X.; et al. Antibacterial Activity of Squaric Amide Derivative SA2 against Methicillin-Resistant Staphylococcus aureus. Antibiotics 2022, 11, 1497. https://doi.org/10.3390/antibiotics11111497
Yu M, Hou Y, Cheng M, Liu Y, Ling C, Zhai D, Zhao H, Li Y, Chen Y, Xue X, et al. Antibacterial Activity of Squaric Amide Derivative SA2 against Methicillin-Resistant Staphylococcus aureus. Antibiotics. 2022; 11(11):1497. https://doi.org/10.3390/antibiotics11111497
Chicago/Turabian StyleYu, Moxi, Yachen Hou, Meiling Cheng, Yongshen Liu, Caise Ling, Dongshen Zhai, Hui Zhao, Yaoyao Li, Yamiao Chen, Xiaoyan Xue, and et al. 2022. "Antibacterial Activity of Squaric Amide Derivative SA2 against Methicillin-Resistant Staphylococcus aureus" Antibiotics 11, no. 11: 1497. https://doi.org/10.3390/antibiotics11111497