In vitro effects of the 4-[(10H-phenothiazin-10-yl)methyl]-N-hydroxybenzamide on Giardia intestinalis trophozoites.

Cytokinesis Cytoskeleton Electron microscopy Giardia intestinalis Lysine deacetylase inhibitor Proliferation

Journal

Acta tropica
ISSN: 1873-6254
Titre abrégé: Acta Trop
Pays: Netherlands
ID NLM: 0370374

Informations de publication

Date de publication:
Aug 2022
Historique:
received: 03 01 2022
revised: 19 04 2022
accepted: 22 04 2022
pubmed: 29 4 2022
medline: 15 6 2022
entrez: 28 4 2022
Statut: ppublish

Résumé

Giardiasis is an intestinal disease caused by the parasite protozoan Giardia intestinalis. For more than five decades, the treatment of this disease has been based on compounds such as nitroimidazoles and benzimidazoles. The parasite's adverse effects and therapeutic failure are largely recognized. Therefore, it is necessary to develop new forms of chemotherapy treatment against giardiasis. Lysine deacetylases (KDACs), which remove an acetyl group from lysine residues in histone and non-histone proteins as tubulin, are found in the Giardia genome and can become an interesting option for giardiasis treatment. In the present study, we evaluated the effects of 4-[(10H-phenothiazin-10-yl)methyl]-N-hydroxybenzamide, a new class I/II KDAC inhibitor, on G. intestinalis growth, cytoskeleton, and ultrastructure organization. This compound decreased parasite proliferation and viability and displayed an IC

Identifiants

pubmed: 35483428
pii: S0001-706X(22)00176-0
doi: 10.1016/j.actatropica.2022.106484
pii:
doi:

Substances chimiques

Lysine K3Z4F929H6

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

106484

Informations de copyright

Copyright © 2022. Published by Elsevier B.V.

Auteurs

Roberta Veríssimo F Oliveira (RVF)

Universidade do Grande Rio (UNIGRANRIO), Rio de Janeiro, RJ, Brazil.

Wanderley de Souza (W)

Laboratório de Ultraestrutura Celular Hertha Meyer, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil; Instituto Nacional de Ciência e Tecnologia em Biologia Estrutural e Bioimagens e Centro Nacional de Biologia Estrutural e Bioimagens, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.

Katharina Vögerl (K)

Department of Pharmacy, Center for Drug Research, Ludwig-Maximilians University, Munich, Germany.

Franz Bracher (F)

Department of Pharmacy, Center for Drug Research, Ludwig-Maximilians University, Munich, Germany.

Marlene Benchimol (M)

Universidade do Grande Rio (UNIGRANRIO), Rio de Janeiro, RJ, Brazil; Laboratório de Ultraestrutura Celular Hertha Meyer, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil; Instituto Nacional de Ciência e Tecnologia em Biologia Estrutural e Bioimagens e Centro Nacional de Biologia Estrutural e Bioimagens, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.

Ana Paula R Gadelha (APR)

Instituto Nacional de Ciência e Tecnologia em Biologia Estrutural e Bioimagens e Centro Nacional de Biologia Estrutural e Bioimagens, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil; Diretoria de Metrologia Aplicada a Ciências da Vida, Instituto Nacional de Metrologia, Qualidade e Tecnologia, Rio de Janeiro, RJ, Brazil. Electronic address: apgadelha@inmetro.gov.br.

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Classifications MeSH