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In Vitro Antibacterial Activity of Rhodanine Derivatives against Pathogenic Clinical Isolates

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dc.contributor.authorAbdelKhalek, Ahmeden
dc.contributor.authorAshby, Charles R.en
dc.contributor.authorPatel, Bhargav A.en
dc.contributor.authorTalele, Tanaji T.en
dc.contributor.authorSeleem, Mohamed N.en
dc.date.accessioned2020-09-21T16:14:53Zen
dc.date.available2020-09-21T16:14:53Zen
dc.date.issued2016-10-06en
dc.date.updated2020-09-21T16:14:51Zen
dc.description.abstractBacterial infections present a serious challenge to healthcare practitioners due to the emergence of resistance to numerous conventional antibacterial drugs. Therefore, new bacterial targets and new antimicrobials are unmet medical needs. Rhodanine derivatives have been shown to possess potent antimicrobial activity via a novel mechanism. However, their potential use as antibacterials has not been fully examined. In this study, we determined the spectrum of activity of seven rhodanine derivatives (compounds Rh 1-7) against clinical isolates of Gram-positive and Gram-negative bacterial strains and Candida albicans. We also synthesized and tested three additional compounds, ethyl ester and amide of rhodanine 2 (Rh 8 and Rh 10, respectively) and ethyl ester of rhodanine 3 (Rh 9) to determine the significance of the carboxyl group modification towards antibacterial activity and human serum albumin binding. A broth microdilution assay confirmed Rh 1-7 exhibit bactericidal activity against Gram-positive pathogens. Rh 2 had significant activity against various vancomycin- resistant (MIC90 = 4 μM) and methicillin-resistant (MIC90 = 4 μM) Staphylococcus aureus (VRSA and MRSA), Staphylococcus epidermidis (MIC = 4 μM) and vancomycinresistant Enterococcus (VRE) strains (MIC90 = 8 μM). The rhodanine compounds exhibited potent activity against Bacillus spp., including Bacillus anthracis, with MIC range of 2-8 μM. In addition, they had potent activity against Clostridium difficile. The most potent compound, Rh 2, at 4 and 8 times its MIC, significantly decreased S. epidermidis biofilm mass by more than 35% and 45%, respectively. None of the rhodanine compounds showed antimicrobial activity (MIC > 128 μM) against various 1) Gram-negative pathogens (Acinetobacter baumannii, Escherichia coli, Klebsiella pneumonia, Pseudomonas aeruginosa, and Salmonella Typhimurium) or 2) strains of Candida albicans (MIC > 64 μM). The MTS assay confirmed that rhodanines were not toxic to mouse murine macrophage (J774.1A) up to 64 μM, human keratinocytes (HaCat) up to 32 μM, and human ileocecal colorectal cell (HRT-18) up to 128 μM. Overall, these data suggest that certain rhodanine compounds may have potential use for the treatment of several multidrug-resistant Gram-positive bacterial infections.en
dc.description.versionPublished versionen
dc.format.extent17 page(s)en
dc.format.mediumElectronic-eCollectionen
dc.format.mimetypeapplication/pdfen
dc.identifierARTN e0164227 (Article number)en
dc.identifier.doihttps://doi.org/10.1371/journal.pone.0164227en
dc.identifier.eissn1932-6203en
dc.identifier.issn1932-6203en
dc.identifier.issue10en
dc.identifier.orcidSeleem, Mohamed [0000-0003-0939-0458]en
dc.identifier.otherPONE-D-16-20080 (PII)en
dc.identifier.pmid27711156 (pubmed)en
dc.identifier.urihttp://hdl.handle.net/10919/100034en
dc.identifier.volume11en
dc.language.isoenen
dc.publisherPLoSen
dc.rightsCreative Commons Attribution 4.0 Internationalen
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.subjectGRAM-NEGATIVE BACTERIAen
dc.subject(Z)-5-ARYLMETHYLIDENE RHODANINESen
dc.subjectSTAPHYLOCOCCAL INFECTIONSen
dc.subjectDAPTOMYCINen
dc.subjectDRUGSen
dc.subject.meshCell Lineen
dc.subject.meshCell Membraneen
dc.subject.meshAnimalsen
dc.subject.meshHumansen
dc.subject.meshMiceen
dc.subject.meshBacteriaen
dc.subject.meshRhodanineen
dc.subject.meshSerum Albuminen
dc.subject.meshAnti-Bacterial Agentsen
dc.subject.meshMicrobial Sensitivity Testsen
dc.subject.meshDrug Resistance, Bacterialen
dc.subject.meshHydrophobic and Hydrophilic Interactionsen
dc.titleIn Vitro Antibacterial Activity of Rhodanine Derivatives against Pathogenic Clinical Isolatesen
dc.title.serialPLOS ONEen
dc.typeArticle - Refereeden
dc.type.dcmitypeTexten
dc.type.otherArticleen
dc.type.otherJournalen
dcterms.dateAccepted2016-09-21en
pubs.organisational-group/Virginia Tech/Veterinary Medicineen
pubs.organisational-group/Virginia Tech/Faculty of Health Sciencesen
pubs.organisational-group/Virginia Tech/All T&R Facultyen
pubs.organisational-group/Virginia Tech/Veterinary Medicine/Biomedical Sciences and Pathobiologyen
pubs.organisational-group/Virginia Tech/Veterinary Medicine/CVM T&R Facultyen
pubs.organisational-group/Virginia Techen

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