首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Trypanothione reductase activity is prominent in metacyclic promastigotes and axenic amastigotes of Leishmania amazonesis. Evaluation of its potential as a therapeutic target.
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Trypanothione reductase activity is prominent in metacyclic promastigotes and axenic amastigotes of Leishmania amazonesis. Evaluation of its potential as a therapeutic target.

机译:锥虫硫磷还原酶活性在利什曼原虫(Leishmania amazonesis)的元环前鞭毛体和轴突性扁桃体中突出。评价其作为治疗靶标的潜力。

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摘要

The activity of trypanothione reductase in Leishmania amazonensis was evaluated and it was demonstrated that TR is expressed in the soluble fractions of infective promastigotes and amastigotes, while non-infective promastigotes expressed the enzyme at basal levels. This data allows an association of enzyme activity and the infective capacity of the parasite. We have also previously demonstrated that amidine compounds (N, N'-diphenyl-4-methoxy-benzamidine and pentamidine) were active against this parasite. Here, experiments concerning the effect of these compounds on TR activity, showed that both compounds significantly inhibited the enzyme. However, against glutathione reductase, only pentamidine showed a significant inhibitory action, suggesting an association with the toxic effects of this drug used in the clinic for the treatment of leishmaniasis.
机译:评估了锥虫硫磷还原酶在亚马逊利什曼原虫中的活性,并证明TR在感染性前鞭毛虫和变形虫的可溶部分中表达,而非感染性前鞭毛虫在基础水平上表达该酶。该数据允许酶活性与寄生虫的感染能力相关联。我们以前也已经证明am化合物(N,N'-二苯基-4-甲氧基-苯甲m和喷他idine)对这种寄生虫具有活性。在这里,有关这些化合物对TR活性影响的实验表明,这两种化合物均显着抑制了该酶。但是,针对谷胱甘肽还原酶,只有喷他idine具有明显的抑制作用,表明与该药物在利什曼病的临床治疗中的毒性作用有关。

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