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Mechanism of antifungal activity by 5-aminoimidazole-4-carbohydrazonamide derivatives against candida albicans and candida krusei

2021Journal article Restricted access
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dc.contributor.authorCerqueira, Fátima
dc.contributor.authorMaia, Marta
dc.contributor.authorGabriel, Carla
dc.contributor.authorMedeiros, R.
dc.contributor.authorCravo, Sara
dc.contributor.authorRibeiro, Ana Isabel
dc.contributor.authorDantas, Daniela
dc.contributor.authorDias, Alice Maria
dc.contributor.authorSaraiva, Lucília
dc.contributor.authorRaimundo, Liliana
dc.contributor.authorPinto, Eugénia
dc.date.accessioned2021-07-13T11:27:06Z
dc.date.available2021-07-13T11:27:06Z
dc.date.issued2021
dc.description.abstractSystemic mycoses are one major cause of morbidity/mortality among immunocompromised/debilitated individuals. Studying the mechanism of action is a strategy to develop safer/potent antifungals, warning resistance emergence. The major goal of this study was to elucidate the mechanism of action of three (Z)-5-amino-N’-aryl-1-methyl-1H-imidazole-4-carbohydrazonamides (2h, 2k, 2l) that had previously demonstrated strong antifungal activity against Candida krusei and C. albicans ATCC strains. Activity was confirmed against clinical isolates, susceptible or resistant to fluconazole by broth microdilution assay. Ergosterol content (HPLC-DAD), mitochondrial dehydrogenase activity (MTT), reactive oxygen species (ROS) generation (flow cytometry), germ tube inhibition and drug interaction were evaluated. None of the compounds inhibited ergosterol synthesis. Ascorbic acid reduced the antifungal effect of compounds and significantly decreased ROS production. The metabolic viability of C. krusei was significantly reduced for values of 2MIC. Compounds 2h and 2k caused a significant increase in ROS production for MIC values while for 2l a significant increase was only observed for concentrations above MIC. ROS production seems to be involved in antifungal activity and the higher activity against C. krusei versus C. albicans may be related to their unequal sensitivity to different ROS. No synergism with fluconazole or amphotericin was observed, but the association of 2h with fluconazole might be valuable due to the significant inhibition of the dimorphic transition, a C. albicans virulence mechanism.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.doi10.3390/antibiotics10020183pt_PT
dc.identifier.eissn2079-6382
dc.identifier.urihttp://hdl.handle.net/10284/10072
dc.language.isoengpt_PT
dc.publisherMDPIpt_PT
dc.subjectCandida sp.pt_PT
dc.subjectAntifungalspt_PT
dc.subject(Z)-5-amino-N’-aryl-1-methyl-1H-imidazole-4-carbohydrazonamidespt_PT
dc.subjectMechanisms of actionpt_PT
dc.subjectReactive oxygen speciespt_PT
dc.subjectErgosterolpt_PT
dc.subjectDimorphic transitionpt_PT
dc.subjectMetabolic viabilitypt_PT
dc.titleMechanism of antifungal activity by 5-aminoimidazole-4-carbohydrazonamide derivatives against candida albicans and candida kruseipt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.issue2pt_PT
oaire.citation.startPage183pt_PT
oaire.citation.titleAntibioticspt_PT
oaire.citation.volume10pt_PT
person.familyNameCerqueira
person.familyNameMedeiros
person.givenNameFátima
person.givenNameRui
person.identifier812695
person.identifier37604
person.identifier.ciencia-idCF14-52ED-5DA0
person.identifier.ciencia-idC51F-5DBE-9C51
person.identifier.orcid0000-0003-4513-4654
person.identifier.orcid0000-0003-3010-8373
person.identifier.ridM-7557-2013
person.identifier.ridC-7938-2009
person.identifier.scopus-author-id6603346911
person.identifier.scopus-author-id7006241641
rcaap.rightsclosedAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublication2705e35c-97f6-4de2-bbf1-d680342760e9
relation.isAuthorOfPublication5ffb7965-d9af-4ba1-a81b-b0aed28de206
relation.isAuthorOfPublication.latestForDiscovery5ffb7965-d9af-4ba1-a81b-b0aed28de206

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