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用于恰加斯病的药物重新利用:尼美舒利对克氏锥虫的体外评估及其作用机制的见解。

Drug repurposing for Chagas disease: In vitro assessment of nimesulide against Trypanosoma cruzi and insights on its mechanisms of action.

作者信息

Trindade Joana D'Arc S, Freire-de-Lima Célio Geraldo, Côrte-Real Suzana, Decote-Ricardo Debora, Freire de Lima Marco Edilson

机构信息

Instituto de Química, Departamento de Química Orgânica, Universidade Federal Rural do Rio de Janeiro, Seropédica, Rio de Janeiro, Brazil.

Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Ilha do Fundão, Rio de Janeiro, Brazil.

出版信息

PLoS One. 2021 Oct 22;16(10):e0258292. doi: 10.1371/journal.pone.0258292. eCollection 2021.

Abstract

Chagas disease is a neglected illness caused by Trypanosoma cruzi and its treatment is done only with two drugs, nifurtimox and benznidazole. However, both drugs are ineffective in the chronic phase, in addition to causing serious side effects. This context of therapeutic limitation justifies the continuous research for alternative drugs. Here, we study the in vitro trypanocidal effects of the non-steroidal anti-inflammatory drug nimesulide, a molecule that has in its chemical structure a toxicophoric nitroaromatic group (NO2). The set of results obtained in this work highlights the potential for repurposing nimesulide in the treatment of this disease that affects millions of people around the world.

摘要

恰加斯病是一种由克氏锥虫引起的被忽视的疾病,其治疗仅使用两种药物,硝呋莫司和苯硝唑。然而,这两种药物在慢性期均无效,此外还会引起严重的副作用。这种治疗局限性的背景证明了对替代药物进行持续研究的合理性。在此,我们研究了非甾体抗炎药尼美舒利的体外杀锥虫作用,该分子在其化学结构中含有一个有毒的硝基芳香基团(NO2)。这项工作中获得的一系列结果凸显了将尼美舒利重新用于治疗这种影响全球数百万人的疾病的潜力。

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