Please use this identifier to cite or link to this item: https://hdl.handle.net/1822/72539

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dc.contributor.authorCerqueira, Fátima-
dc.contributor.authorMaia, Marta-
dc.contributor.authorGabriel, Carla-
dc.contributor.authorMedeiros, Rui-
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.accessioned2021-05-06T13:10:01Z-
dc.date.available2021-05-06T13:10:01Z-
dc.date.issued2021-
dc.identifier.citationCerqueira, F.; Maia, M.; Gabriel, C.; Medeiros, R.; Cravo, S.; Ribeiro, A.I.; Dantas, D.; Dias, A.M.; Saraiva, L.; Raimundo, L.; Pinto, E. Mechanism of Antifungal Activity by 5-Aminoimidazole-4-Carbohydrazonamide Derivatives against Candida albicans and Candida krusei. Antibiotics 2021, 10, 183. https://doi.org/10.3390/antibiotics10020183-
dc.identifier.issn2079-6382por
dc.identifier.urihttps://hdl.handle.net/1822/72539-
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 (<i>Z</i>)-5-amino-<i>N</i>’-aryl-1-methyl-1<i>H</i>-imidazole-4-carbohydrazonamides (2h, 2k, 2l) that had previously demonstrated strong antifungal activity against <i>Candida krusei</i> and <i>C. albicans</i> 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 <i>C. krusei</i> 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 <i>C. krusei</i> versus <i>C. albicans</i> 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 <i>C. albicans</i> virulence mechanism.-
dc.description.sponsorshipThis research was partially supported by national funds through FCT—Foundation for Sci ence and Technology within the scope of UID/Multi/04546/2019, UIDB/04423/2020, UIDB/50006/2020, UID/QUI/00686/2020.-
dc.language.isoeng-
dc.publisherMultidisciplinary Digital Publishing Institute-
dc.relationUID/Multi/04546/2019-
dc.relationUIDB/04423/2020-
dc.relationUIDB/50006/2020-
dc.relationUID/QUI/00686/2020-
dc.rightsopenAccess-
dc.subjectCandida sppor
dc.subjectantifungalspor
dc.subject(Z)-5-amino-N&#8217por
dc.subject-aryl-1-methyl-1H-imidazole-4-carbohydrazonamidespor
dc.subjectmechanisms of actionpor
dc.subjectreactive oxygen speciespor
dc.subjectergosterolpor
dc.subjectdimorphic transitionpor
dc.subjectmetabolic viabilitypor
dc.subject(Z)-5-amino-N’-aryl-1-methyl-1H-imidazole-4-carbohydrazonamidespor
dc.titleMechanism of Antifungal Activity by 5-Aminoimidazole-4-Carbohydrazonamide Derivatives against Candida albicans and Candida krusei-
dc.typearticle-
dc.relation.publisherversionhttps://www.mdpi.com/2079-6382/10/2/183-
oaire.citationStartPage1por
oaire.citationEndPage13por
oaire.citationIssue2por
oaire.citationVolume10por
dc.date.updated2021-03-12T14:38:20Z-
dc.identifier.eissn2079-6382-
dc.identifier.doi10.3390/antibiotics10020183-
dc.subject.wosScience & Technologypor
sdum.journalAntibiotics-
Appears in Collections:CDQuim - Artigos (Papers)

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