Inhibition of Trypanosoma cruzi trypanothione reductase by crystal violet

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 H 2O 2. The trypanocidal drug crystal violet wa...

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Veröffentlicht in:Molecular and biochemical parasitology 1994-10, Vol.67 (2), p.313-320
Hauptverfasser: Moreno, Silvia N.J., Carnieri, Eva G.S., Docampo, Roberto
Format: Artikel
Sprache:eng
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Zusammenfassung: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 H 2O 2. 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 K i of 5.3 ± 0.5 μM, 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.
ISSN:0166-6851
1872-9428
DOI:10.1016/0166-6851(94)00140-5