دورية أكاديمية
AMXT-1501 targets membrane phospholipids against Gram-positive and -negative multidrug-resistant bacteria
| العنوان: | AMXT-1501 targets membrane phospholipids against Gram-positive and -negative multidrug-resistant bacteria |
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| المؤلفون: | Jinxin Zheng, Xiaoju Liu, Yanpeng Xiong, Qingyin Meng, Peiyu Li, Fan Zhang, Xiaoming Liu, Zhiwei Lin, Qiwen Deng, Zewen Wen, Zhijian Yu |
| المصدر: | Emerging Microbes and Infections, Vol 13, Iss 1 (2024) |
| بيانات النشر: | Taylor & Francis Group, 2024. |
| سنة النشر: | 2024 |
| المجموعة: | LCC:Infectious and parasitic diseases LCC:Microbiology |
| مصطلحات موضوعية: | Multidrug-resistant, MRSA, ESBL, CRE, AMXT-1501, Cardiolipin, Infectious and parasitic diseases, RC109-216, Microbiology, QR1-502 |
| الوصف: | ABSTRACTThe rapid proliferation of multidrug-resistant (MDR) bacterial pathogens poses a serious threat to healthcare worldwide. Carbapenem-resistant (CR) Enterobacteriaceae, which have near-universal resistance to available antimicrobials, represent a particularly concerning issue. Herein, we report the identification of AMXT-1501, a polyamine transport system inhibitor with antibacterial activity against Gram-positive and -negative MDR bacteria. We observed minimum inhibitory concentration (MIC)50/MIC90 values for AMXT-1501 in the range of 3.13–12.5 μM (2.24–8.93 μg /mL), including for methicillin-resistant Staphylococcus aureus (MRSA), CR Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. AMXT-1501 was more effective against MRSA and CR E. coli than vancomycin and tigecycline, respectively. Subinhibitory concentrations of AMXT-1501 reduced the biofilm formation of S. aureus and Enterococcus faecalis. Mechanistically, AMXT-1501 exposure damaged microbial membranes and increased membrane permeability and membrane potential by binding to cardiolipin (CL) and phosphatidylglycerol (PG). Importantly, AMXT-1501 pressure did not induce resistance readily in the tested pathogens. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 22221751 2222-1751 |
| Relation: | https://doaj.org/toc/2222-1751 |
| DOI: | 10.1080/22221751.2024.2321981 |
| URL الوصول: | https://doaj.org/article/42875b07299b49d5897c2de02a19cc54 |
| رقم الأكسشن: | edsdoj.42875b07299b49d5897c2de02a19cc54 |
| قاعدة البيانات: | Directory of Open Access Journals |
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Full Text Finder | تدمد: | 22221751 |
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| DOI: | 10.1080/22221751.2024.2321981 |