Tolnaftate inhibits ergosterol production and impacts cell viability of Leishmania sp.
Anti-fungal drug
Cell membrane
Drug repurposing
Ergosterol
Mechanism of action
Mitochondria
New World Leishmaniasis
Tolnaftate
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
09 2020
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
104056Informations 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.