Literature DB >> 7870135

Inhibition of Trypanosoma cruzi trypanothione reductase by crystal violet.

S N Moreno1, E G Carnieri, R Docampo.   

Abstract

A trypanothione reductase activity is present in all the main differentiation stages of Trypanosoma cruzi, amastigotes having the highest activity, and trypomastigotes the lowest. Trypanothione reductase could not be induced in epimastigotes exposed to H2O2. The trypanocidal drug crystal violet was a potent inhibitor of T. cruzi trypanothione reductase in vitro. The inhibition was competitive with respect to trypanothione with a Ki of 5.3 +/- 0.5 microM, uncompetitive with NADPH, and increased below pH 7.0 and above pH 8.0. Crystal violet, however, was not able to decrease the level of total reduced thiols in intact cells. Dihydrotrypanothione but not reduced glutathione, protected the enzyme from inhibition by crystal violet.

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Year:  1994        PMID: 7870135     DOI: 10.1016/0166-6851(94)00140-5

Source DB:  PubMed          Journal:  Mol Biochem Parasitol        ISSN: 0166-6851            Impact factor:   1.759


  5 in total

Review 1.  Parasite-specific trypanothione reductase as a drug target molecule.

Authors:  R Luise Krauth-Siegel; Oliver Inhoff
Journal:  Parasitol Res       Date:  2003-04-23       Impact factor: 2.289

2.  Oxyrane derivative of alpha-lapachone is potent growth inhibitor of Trypanosoma cruzi epimastigote forms.

Authors:  Alessandra Jorqueira; Robson M Gouvêa; Vitor F Ferreira; Milton N da Silva; Maria C B V de Souza; Aline A Zuma; Danielle F B Cavalcanti; Humberto P Araújo; Dilvani O Santos; Saulo C Bourguignon
Journal:  Parasitol Res       Date:  2006-04-05       Impact factor: 2.383

Review 3.  Advances in preclinical approaches to Chagas disease drug discovery.

Authors:  Fernando Villalta; Girish Rachakonda
Journal:  Expert Opin Drug Discov       Date:  2019-08-14       Impact factor: 6.098

4.  Improved tricyclic inhibitors of trypanothione reductase by screening and chemical synthesis.

Authors:  John L Richardson; Isabelle R E Nett; Deuan C Jones; Mohamed H Abdille; Ian H Gilbert; Alan H Fairlamb
Journal:  ChemMedChem       Date:  2009-08       Impact factor: 3.466

Review 5.  Mitochondrial Ca2+ and Reactive Oxygen Species in Trypanosomatids.

Authors:  Roberto Docampo; Aníbal Eugénio Vercesi
Journal:  Antioxid Redox Signal       Date:  2021-09-17       Impact factor: 7.468

  5 in total

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