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结晶紫对克氏锥虫锥虫硫醇还原酶的抑制作用。

Inhibition of Trypanosoma cruzi trypanothione reductase by crystal violet.

作者信息

Moreno S N, Carnieri E G, Docampo R

机构信息

Department of Veterinary Pathobiology, University of Illinois at Urbana-Champaign 61801.

出版信息

Mol Biochem Parasitol. 1994 Oct;67(2):313-20. doi: 10.1016/0166-6851(94)00140-5.

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.

摘要

克鲁斯锥虫的所有主要分化阶段均存在锥虫硫醇还原酶活性,无鞭毛体的活性最高,而 trypomastigotes 的活性最低。暴露于 H2O2 的上鞭毛体中无法诱导出锥虫硫醇还原酶。杀锥虫药物结晶紫在体外是克鲁斯锥虫锥虫硫醇还原酶的有效抑制剂。该抑制作用对锥虫硫醇具有竞争性,Ki 为 5.3 +/- 0.5 microM,对 NADPH 无竞争性,且在 pH 7.0 以下和 pH 8.0 以上时增强。然而,结晶紫无法降低完整细胞中总还原硫醇的水平。二氢锥虫硫醇而非还原型谷胱甘肽可保护该酶免受结晶紫的抑制。

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