Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 김우성 | * |
dc.date.accessioned | 2020-12-03T16:30:13Z | - |
dc.date.available | 2020-12-03T16:30:13Z | - |
dc.date.issued | 2020 | * |
dc.identifier.issn | 2079-6382 | * |
dc.identifier.other | OAK-28234 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/255556 | - |
dc.description.abstract | Multidrug-resistant pathogens pose a serious threat to human health. For decades, the antibiotic vancomycin has been a potent option when treating Gram-positive multidrug-resistant infections. Nonetheless, in recent decades, we have begun to see an increase in vancomycin-resistant bacteria. Here, we show that the nuclear factor-kappa B (NF-κB) inhibitor N-[3,5Bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide (IMD0354) was identified as a positive hit through a Caenorhabditis elegans–methicillin-resistant Staphylococcus aureus (MRSA) infection screen. IMD0354 was a potent bacteriostatic drug capable of working at a minimal inhibitory concentration (MIC) as low as 0.06 µg/mL against various vancomycin-resistant strains. Interestingly, IMD0354 showed no hemolytic activity at concentrations as high as 16 µg/mL and is minimally toxic to C. elegans in vivo with 90% survival up to 64 µg/mL. In addition, we demonstrated that IMD0354′s mechanism of action at high concentrations is membrane permeabilization. Lastly, we found that IMD0354 is able to inhibit vancomycin-resistant Staphylococcus aureus (VRSA) initial cell attachment and biofilm formation at sub-MIC levels and above. Our work highlights that the NF-κB inhibitor IMD0354 has promising potential as a lead compound and an antimicrobial therapeutic candidate capable of combating multidrug-resistant bacteria. © 2020 by the authors. Licensee MDPI, Basel, Switzerland. | * |
dc.language | English | * |
dc.publisher | MDPI AG | * |
dc.subject | High-throughput screening | * |
dc.subject | IMD0354 | * |
dc.subject | Vancomycin-resistant Staphylococcus aureus | * |
dc.subject | Vancomycinresistant enterococci | * |
dc.title | New antimicrobial bioactivity against multidrugresistant gram-positive bacteria of kinase inhibitor imd0354 | * |
dc.type | Article | * |
dc.relation.issue | 10 | * |
dc.relation.volume | 9 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 1 | * |
dc.relation.lastpage | 17 | * |
dc.relation.journaltitle | Antibiotics | * |
dc.identifier.doi | 10.3390/antibiotics9100665 | * |
dc.identifier.wosid | WOS:000584134000001 | * |
dc.identifier.scopusid | 2-s2.0-85092044299 | * |
dc.author.google | Escobar I.E. | * |
dc.author.google | White A. | * |
dc.author.google | Kim W. | * |
dc.author.google | Mylonakis E. | * |
dc.contributor.scopusid | 김우성(57201881427) | * |
dc.date.modifydate | 20240603112237 | * |