Rotenone enhances antifungal activity of novel pyrazoles against Candida spp.

Detalhes bibliográficos
Autor(a) principal: Quejada, Luis Fernando
Data de Publicação: 2022
Outros Autores: Almeida, Renata de, Vegi, Percilene Fazolin, Santos, Maurício Silva dos, Bernardino, Alice Maria Rolim, Vericimo, Mauricio Afonso, Faria, Robson Xavier
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/56243
Resumo: Proteomics and Human Mycosis Unit, Group of Infectious Diseases Department of Microbiology, Faculty of Sciences, Pontificia Universidad Javeriana, Carrera 7 No. 43- 82, Bogota, D.C, 110231, Colombia / Laboratory of Immunology and Infectious and Granulomatous Diseases, Department of Biology, Fluminense Federal University, Niterói, RJ, Brazil / Postgraduate Program in Science and Biotechnology, Fluminense Federal University, Niterói, RJ, Brazil.
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spelling Quejada, Luis FernandoAlmeida, Renata deVegi, Percilene FazolinSantos, Maurício Silva dosBernardino, Alice Maria RolimVericimo, Mauricio AfonsoFaria, Robson Xavier2023-01-01T13:51:52Z2023-01-01T13:51:52Z2022QUEJADA, Luis Fernando et al. Rotenone enhances antifungal activity of novel pyrazoles against Candida spp. European Journal of Medicinal Chemistry Reports, 5, 100045, p. 1 - 9, Apr. 2022.2772-4174https://www.arca.fiocruz.br/handle/icict/5624310.1016/j.ejmcr.2022.100045engElsevier Masson SAS.Micoses invasivasCândidaPirazóisImidazolinasRetenonaAntifúngicosInvasive mycosesCandidaPyrazolesImidazolinesRotenoneAntifungalsRotenone enhances antifungal activity of novel pyrazoles against Candida spp.info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleProteomics and Human Mycosis Unit, Group of Infectious Diseases Department of Microbiology, Faculty of Sciences, Pontificia Universidad Javeriana, Carrera 7 No. 43- 82, Bogota, D.C, 110231, Colombia / Laboratory of Immunology and Infectious and Granulomatous Diseases, Department of Biology, Fluminense Federal University, Niterói, RJ, Brazil / Postgraduate Program in Science and Biotechnology, Fluminense Federal University, Niterói, RJ, Brazil.Laboratory of Immunology and Infectious and Granulomatous Diseases, Department of Biology, Fluminense Federal University, Niterói, RJ, Brazil / Postgraduate Program in Pathology, Fluminense Federal University, Niterói, RJ, BrazilPostgraduate Program in Chemistry, Institute of Chemistry, Fluminense Federal University, Niterói, RJ, Brazil.Multicentric Postgraduate Program in Chemistry (PPGMQ-MG), Institute of Physics and Chemistry, Federal University of Itajubá, Itajubá, MG, Brazil.Postgraduate Program in Chemistry, Institute of Chemistry, Fluminense Federal University, Niterói, RJ, Brazil.Laboratory of Immunology and Infectious and Granulomatous Diseases, Department of Biology, Fluminense Federal University, Niterói, RJ, Brazil / Postgraduate Program in Science and Biotechnology, Fluminense Federal University, Niterói, RJ, Brazil.Postgraduate Program in Chemistry, Institute of Chemistry, Fluminense Federal University, Niterói, RJ, Brazil. / Toxoplasmosis and other Protozoa Laboratory, Oswaldo Cruz Institute, Oswaldo Cruz Foundation-FIOCRUZ. Rio de Janeiro, RJ, Brasil.Mycoses annually affect about 2 million individuals worldwide, especially in tropical countries. Candida spp., one of the main etiologic agents of these mycoses, and in particular Candida albicans has been the most isolated pathogen in patients with severe clinical cases of invasive candidiasis and candidemia, causing frequent infections or opportunistic and chronic systemic forms. However, the emergence of non-albicans infections has become a public health concern worldwide. In discovering har.mless molecules, the pyrazoles have attracted many scientists because their great synthetic versatility and extensive therapeutic properties such as antibacterials, antivirals, antimalarials, and anti-inflammatories, anti-leishmaniasis, and antifungals. They are part of Azole compounds used for decades for antifungal treatment. The azole action mechanism is related to ergosterol synthesis inhibition by blocking the target enzymes, known as Erg11p, leading to fungistatic action. We evaluated the antifungal potential of 12 pyrazole derivatives. Compound 1d caused prominent action against Candida glabrata. Thus, we employed Rotenone as a mitochondrial complex I inhibitor. Rotenone helped to enhance the effect of the novel pyrazole derivatives tested against Candida spp, decreasing MICs value from a range of 250–500 to <3.1 μg/mL. Pyrazoles had a reduced cytotoxicity effect on in vivo cell culture than ketoconazole. Although ROS production might be a possible mechanism, it remained unclear. Thus, new studies must elucidate this synergistic action.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/56243/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALRobsonXFaria_LuisQuejada_etal_IOC_2022.pdfRobsonXFaria_LuisQuejada_etal_IOC_2022.pdfapplication/pdf1397644https://www.arca.fiocruz.br/bitstream/icict/56243/2/RobsonXFaria_LuisQuejada_etal_IOC_2022.pdfd98b8be819805e459ce6194e2d1093f8MD52icict/562432023-09-04 11:03:27.841oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352023-09-04T14:03:27Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.en_US.fl_str_mv Rotenone enhances antifungal activity of novel pyrazoles against Candida spp.
title Rotenone enhances antifungal activity of novel pyrazoles against Candida spp.
spellingShingle Rotenone enhances antifungal activity of novel pyrazoles against Candida spp.
Quejada, Luis Fernando
Micoses invasivas
Cândida
Pirazóis
Imidazolinas
Retenona
Antifúngicos
Invasive mycoses
Candida
Pyrazoles
Imidazolines
Rotenone
Antifungals
title_short Rotenone enhances antifungal activity of novel pyrazoles against Candida spp.
title_full Rotenone enhances antifungal activity of novel pyrazoles against Candida spp.
title_fullStr Rotenone enhances antifungal activity of novel pyrazoles against Candida spp.
title_full_unstemmed Rotenone enhances antifungal activity of novel pyrazoles against Candida spp.
title_sort Rotenone enhances antifungal activity of novel pyrazoles against Candida spp.
author Quejada, Luis Fernando
author_facet Quejada, Luis Fernando
Almeida, Renata de
Vegi, Percilene Fazolin
Santos, Maurício Silva dos
Bernardino, Alice Maria Rolim
Vericimo, Mauricio Afonso
Faria, Robson Xavier
author_role author
author2 Almeida, Renata de
Vegi, Percilene Fazolin
Santos, Maurício Silva dos
Bernardino, Alice Maria Rolim
Vericimo, Mauricio Afonso
Faria, Robson Xavier
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Quejada, Luis Fernando
Almeida, Renata de
Vegi, Percilene Fazolin
Santos, Maurício Silva dos
Bernardino, Alice Maria Rolim
Vericimo, Mauricio Afonso
Faria, Robson Xavier
dc.subject.other.en_US.fl_str_mv Micoses invasivas
Cândida
Pirazóis
Imidazolinas
Retenona
Antifúngicos
topic Micoses invasivas
Cândida
Pirazóis
Imidazolinas
Retenona
Antifúngicos
Invasive mycoses
Candida
Pyrazoles
Imidazolines
Rotenone
Antifungals
dc.subject.en.en_US.fl_str_mv Invasive mycoses
Candida
Pyrazoles
Imidazolines
Rotenone
Antifungals
description Proteomics and Human Mycosis Unit, Group of Infectious Diseases Department of Microbiology, Faculty of Sciences, Pontificia Universidad Javeriana, Carrera 7 No. 43- 82, Bogota, D.C, 110231, Colombia / Laboratory of Immunology and Infectious and Granulomatous Diseases, Department of Biology, Fluminense Federal University, Niterói, RJ, Brazil / Postgraduate Program in Science and Biotechnology, Fluminense Federal University, Niterói, RJ, Brazil.
publishDate 2022
dc.date.issued.fl_str_mv 2022
dc.date.accessioned.fl_str_mv 2023-01-01T13:51:52Z
dc.date.available.fl_str_mv 2023-01-01T13:51:52Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.citation.fl_str_mv QUEJADA, Luis Fernando et al. Rotenone enhances antifungal activity of novel pyrazoles against Candida spp. European Journal of Medicinal Chemistry Reports, 5, 100045, p. 1 - 9, Apr. 2022.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/56243
dc.identifier.issn.en_US.fl_str_mv 2772-4174
dc.identifier.doi.none.fl_str_mv 10.1016/j.ejmcr.2022.100045
identifier_str_mv QUEJADA, Luis Fernando et al. Rotenone enhances antifungal activity of novel pyrazoles against Candida spp. European Journal of Medicinal Chemistry Reports, 5, 100045, p. 1 - 9, Apr. 2022.
2772-4174
10.1016/j.ejmcr.2022.100045
url https://www.arca.fiocruz.br/handle/icict/56243
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier Masson SAS.
publisher.none.fl_str_mv Elsevier Masson SAS.
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
bitstream.url.fl_str_mv https://www.arca.fiocruz.br/bitstream/icict/56243/1/license.txt
https://www.arca.fiocruz.br/bitstream/icict/56243/2/RobsonXFaria_LuisQuejada_etal_IOC_2022.pdf
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