Tolnaftate inhibits ergosterol production and impacts cell viability of Leishmania sp.


Journal

Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703

Informations de publication

Date de publication:
09 2020
Historique:
received: 11 05 2020
revised: 12 06 2020
accepted: 26 06 2020
pubmed: 13 7 2020
medline: 9 3 2021
entrez: 13 7 2020
Statut: ppublish

Résumé

Leishmaniasis is an infectious disease caused by protozoan parasites of the genus Leishmania. The treatment of all forms of leishmaniasis relies on first-line drug, pentavalent antimonial, and in cases of drug failure, the second-line drug amphotericin B has been used. Besides the high toxicity of drugs, parasites can be resistant to antimonial in some areas of the World, making it necessary to perform further studies for the characterization of new antileishmanial agents. Thus, the aim of the present work was to evaluate the leishmanicidal activity of tolnaftate, a selective reversible and non-competitive inhibitor of the fungal enzyme squalene epoxidase, which is involved in the biosynthesis of ergosterol, essential to maintain membrane physiology in fungi as well as trypanosomatids. Tolnaftate eliminated promastigote forms of L. (L.) amazonensis, L. (V.) braziliensis and L. (L.) infantum (EC

Identifiants

pubmed: 32653607
pii: S0045-2068(20)31353-5
doi: 10.1016/j.bioorg.2020.104056
pii:
doi:

Substances chimiques

Antifungal Agents 0
Antiprotozoal Agents 0
Tolnaftate 06KB629TKV
Ergosterol Z30RAY509F

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

104056

Informations de copyright

Copyright © 2020 Elsevier Inc. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Eduardo Seiji Yamamoto (ES)

Laboratory of Pathology of Infectious Diseases (LIM50), Department of Pathology, Medical School of São Paulo University, Av. Dr. Arnaldo, 455, Cerqueira César, São Paulo 01246-903, SP, Brazil.

Jéssica Adriana de Jesus (JA)

Laboratory of Pathology of Infectious Diseases (LIM50), Department of Pathology, Medical School of São Paulo University, Av. Dr. Arnaldo, 455, Cerqueira César, São Paulo 01246-903, SP, Brazil.

Adriana Bezerra-Souza (A)

Laboratory of Pathology of Infectious Diseases (LIM50), Department of Pathology, Medical School of São Paulo University, Av. Dr. Arnaldo, 455, Cerqueira César, São Paulo 01246-903, SP, Brazil.

Juliana R Brito (JR)

Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, 09210-180 São Paulo, Brazil.

João Henrique G Lago (JHG)

Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, 09210-180 São Paulo, Brazil.

Márcia Dalastra Laurenti (MD)

Laboratory of Pathology of Infectious Diseases (LIM50), Department of Pathology, Medical School of São Paulo University, Av. Dr. Arnaldo, 455, Cerqueira César, São Paulo 01246-903, SP, Brazil.

Luiz Felipe Domingues Passero (LFD)

São Paulo State University (UNESP), Institute of Biosciences, São Vicente, Praça Infante Dom Henrique, s/n, 11330-900 São Vicente, SP, Brazil; São Paulo State University (UNESP), Institute for Advanced Studies of Ocean, São Vicente, Av. João Francisco Bensdorp, 1178, 11350-011 São Vicente, SP, Brazil. Electronic address: felipe.passero@unesp.br.

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Classifications MeSH