Thiosemicarbazone of lapachol acts on cell membrane in Paracoccidioides brasiliensis

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dc.creatorNívea Pereira de Sá
dc.creatorPatrícia Silva Cisalpino
dc.creatorCaryne Margotto Bertollo
dc.creatorPatrícia Campi Santos
dc.creatorCarlos Augusto Rosa
dc.creatorDaniele da Glória de Souza
dc.creatorPaulo Jorge Sanches Barbeira
dc.creatorTânia Maria de Almeida Alves
dc.creatorCarlos Leomar Zani
dc.creatorSusana Johann
dc.date.accessioned2024-04-19T12:53:37Z
dc.date.accessioned2025-09-09T01:27:36Z
dc.date.available2024-04-19T12:53:37Z
dc.date.issued2019
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Gerais
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
dc.identifier.doihttps://doi.org/10.1093/mmy/myy045
dc.identifier.issn1460-2709
dc.identifier.urihttps://hdl.handle.net/1843/67451
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofMedical Mycology
dc.rightsAcesso Restrito
dc.subjectFungos
dc.subjectCelulas - Membranas
dc.subjectAntimicotico
dc.subjectAtividade antifúngica
dc.subjectParacoccidioides brasiliensis
dc.subjectMicoses sistêmicas
dc.subjectProdutos de ação antimicrobiana
dc.subject.otherAntifungal
dc.subject.otherErgosterol
dc.subject.otherThiosemicarbazone of lapachol
dc.subject.otherParacoccidioides
dc.titleThiosemicarbazone of lapachol acts on cell membrane in Paracoccidioides brasiliensis
dc.typeArtigo de periódico
local.citation.epage339
local.citation.issue3
local.citation.spage332
local.citation.volume57
local.description.resumoParacoccidioidomycosis (PCM) is the most prevalent systemic mycosis in Latin American countries. Amphotericin B, sulfonamides, and azoles may be used in the treatment of PCM. However, the high toxicity, prolonged course of treatment, and significant frequency of disease relapse compromise their use. Therefore, there is a need to seek new therapeutic options. We conducted tests with thiosemicarbazone of lapachol (TSC-lap) to determine the antifungal activity and phenotypic effects against several isolates of Paracoccidioides spp. In addition, we evaluated the toxicity against murine macrophages and the ability to enhance phagocytosis. Further, we verified that TSC-lap was active against yeasts but did not show any interaction with the drugs tested. The TSC-lap showed no toxicity at the concentration of 40 μg/ml in macrophages, and at 15.6 μg/ml it could increase the phagocytic index. We observed that this compound induced in vitro ultrastructural changes manifested as withered and broken cells beyond a disorganized cytoplasm with accumulation of granules. We did not observe indications of activity in the cell wall, although membrane damages were noted. We observed alterations in the membrane permeability, culminating in a significant increase in K+ efflux and a gradual loss of the cellular content with increase in the concentration of TSC-lap. In addition, we showed a significant reduction of ergosterol amount in the Pb18 membrane. These data reinforce the possible mechanism of action of this compound to be closely associated with ergosterol biosynthesis and reaffirms the antifungal potential of TSC-lap against Paracoccidioidesspp.
local.identifier.orcidhttps://orcid.org/0000-0002-4115-559X
local.identifier.orcidhttps://orcid.org/0000-0002-0056-9075
local.identifier.orcidhttps://orcid.org/0000-0002-7478-5934
local.identifier.orcidhttps://orcid.org/0000-0002-0770-8680
local.identifier.orcidhttps://orcid.org/0000-0002-0582-3968
local.identifier.orcidhttps://orcid.org/0000-0003-1859-177X
local.identifier.orcidhttps://orcid.org/0000-0001-8068-1720
local.publisher.countryBrasil
local.publisher.departmentICB - DEPARTAMENTO DE MICROBIOLOGIA
local.publisher.departmentICX - DEPARTAMENTO DE QUÍMICA
local.publisher.initialsUFMG
local.url.externahttps://academic.oup.com/mmy/article/57/3/332/5045352

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