New insights on Ethambutol Targets in Mycobacterium tuberculosis.


Journal

Infectious disorders drug targets
ISSN: 2212-3989
Titre abrégé: Infect Disord Drug Targets
Pays: United Arab Emirates
ID NLM: 101269158

Informations de publication

Date de publication:
2019
Historique:
received: 28 06 2017
revised: 18 01 2018
accepted: 22 01 2018
pubmed: 26 1 2018
medline: 7 6 2019
entrez: 26 1 2018
Statut: ppublish

Résumé

In recent years, very few effective drugs against Mycobacterium tuberculosis have emerged, which motivates the research with drugs already used in the treatment of tuberculosis. Ethambutol is a bacteriostatic drug that affects cell wall integrity, but the effects of this drug on bacilli are not fully exploited. Based on the need to better investigate the complex mechanism of action of ethambutol, our study presented the proteome profile of M. tuberculosis after different times of ethambutol exposure, aiming to comprehend the dynamics of bacilli response to its effects. M. tuberculosis was exposed to ½ MIC of ethambutol at 24 and 48 hours. The proteins were identified by MALDI-TOF/TOF. The main protein changes occurred in metabolic proteins as dihydrolipoyl dehydrogenase (Rv0462), glutamine synthetase1 (Rv2220), electron transfer flavoprotein subunit beta (Rv3029c) and adenosylhomocysteinase (Rv3248c). Considering the functions of these proteins, our results support that the intermediary metabolism and respiration were affected by ethambutol and this disturbance provided proteins that could be explored as additional targets for this drug.

Sections du résumé

BACKGROUND BACKGROUND
In recent years, very few effective drugs against Mycobacterium tuberculosis have emerged, which motivates the research with drugs already used in the treatment of tuberculosis. Ethambutol is a bacteriostatic drug that affects cell wall integrity, but the effects of this drug on bacilli are not fully exploited.
OBJECTIVE OBJECTIVE
Based on the need to better investigate the complex mechanism of action of ethambutol, our study presented the proteome profile of M. tuberculosis after different times of ethambutol exposure, aiming to comprehend the dynamics of bacilli response to its effects. M. tuberculosis was exposed to ½ MIC of ethambutol at 24 and 48 hours. The proteins were identified by MALDI-TOF/TOF.
RESULTS RESULTS
The main protein changes occurred in metabolic proteins as dihydrolipoyl dehydrogenase (Rv0462), glutamine synthetase1 (Rv2220), electron transfer flavoprotein subunit beta (Rv3029c) and adenosylhomocysteinase (Rv3248c).
CONCLUSION CONCLUSIONS
Considering the functions of these proteins, our results support that the intermediary metabolism and respiration were affected by ethambutol and this disturbance provided proteins that could be explored as additional targets for this drug.

Identifiants

pubmed: 29366429
pii: IDDT-EPUB-88174
doi: 10.2174/1871526518666180124140840
doi:

Substances chimiques

Antitubercular Agents 0
Bacterial Proteins 0
Proteome 0
Ethambutol 8G167061QZ

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

73-80

Informations de copyright

Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

Auteurs

Luciana D Ghiraldi-Lopes (LD)

Universidade Estadual de Maringa - Departamento de Analises Clinicas e Biomedicina, Maringa, Parana, Brazil.

Paula A Zanetti Campanerut-Sá (PAZ)

Universidade Estadual de Maringa - Departamento de Analises Clinicas e Biomedicina, Maringa, Parana, Brazil.

Geisa P Caprini Evaristo (GPC)

Laboratorio de Apoio ao Desenvolvimento Tecnologico - Instituto de Quimica, Rio de Janeiro, Rio de Janeiro, Brazil.

Jean E Meneguello (JE)

Universidade Estadual de Maringa - Departamento de Analises Clinicas e Biomedicina, Maringa, Parana, Brazil.

Adriana Fiorini (A)

Universidade Estadual de Maringa - Departamento de Analises Clinicas e Biomedicina, Maringa, Parana, Brazil.

Vanessa P Baldin (VP)

Universidade Estadual de Maringa - Departamento de Analises Clinicas e Biomedicina, Maringa, Parana, Brazil.

Emanuel Maltempi de Souza (EM)

Universidade Federal do Parana - Departamento de Ciencias Biologicas, Curitiba, Parana, Brazil.

Regiane Bertin de Lima Scodro (RB)

Universidade Estadual de Maringa - Departamento de Analises Clinicas e Biomedicina, Maringa, Parana, Brazil.

Vera L D Siqueira (VLD)

Universidade Estadual de Maringa - Departamento de Analises Clinicas e Biomedicina, Maringa, Parana, Brazil.

Rosilene F Cardoso (RF)

Universidade Estadual de Maringa - Departamento de Analises Clinicas e Biomedicina, Maringa, Parana, Brazil.

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Classifications MeSH