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体外评价抗疟药青蒿琥酯对人淋巴细胞的遗传毒性和细胞毒性。

In vitro evaluation of the genotoxic and cytotoxic effects of artesunate, an antimalarial drug, in human lymphocytes.

机构信息

Laboratório de Citogenética Humana, Instituto de Ciências Biológicas, Universidade Federal do Pará (UFPA), Belém - Pará - Brazil.

出版信息

Environ Mol Mutagen. 2011 Aug;52(7):590-4. doi: 10.1002/em.20659. Epub 2011 Jul 4.

Abstract

Artesunate is one of the main antimalarial drugs used in several countries. It is a semisynthetic compound derived from artemisinin, a substance extracted from the Chinese plant, Artemisia annua L. Despite the widespread use of artesunate as an antimalarial drug, there is a lack of data regarding its genotoxic effects in human lymphocytes. Therefore, in this study, we used the comet assay and micronucleus test to evaluate the possible genotoxic effects of artesunate in cultured human lymphocytes. In addition, cell death by necrosis and apoptosis was also assessed. Cells exposed to different concentrations of artesunate showed a significant concentration-dependent increase (P < 0.05) in DNA damage index and micronuclei frequency. A significant increase in the frequency of apoptotic and necrotic cells was also observed. Our results showed that artesunate is a genotoxic and cytotoxic compound in cultured human lymphocytes.

摘要

青蒿琥酯是几种国家中使用的主要抗疟药物之一。它是一种从青蒿素中提取的半合成化合物,青蒿素是从中国植物黄花蒿中提取的物质。尽管青蒿琥酯作为抗疟药物广泛使用,但关于其在人类淋巴细胞中的遗传毒性作用的数据仍然缺乏。因此,在这项研究中,我们使用彗星试验和微核试验来评估青蒿琥酯在培养的人类淋巴细胞中的可能遗传毒性作用。此外,还评估了细胞坏死和细胞凋亡导致的细胞死亡。暴露于不同浓度青蒿琥酯的细胞显示出 DNA 损伤指数和微核频率的显著浓度依赖性增加(P < 0.05)。凋亡和坏死细胞的频率也显著增加。我们的结果表明,青蒿琥酯是一种在培养的人类淋巴细胞中具有遗传毒性和细胞毒性的化合物。

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