蒿甲醚抗利什曼原虫活性及毒性的体外评价：聚焦其凋亡效应
In-vitro Evaluation of Antileishmanial Activity and Toxicity of Artemether with Focus on its Apoptotic Effect.
作者信息
Ebrahimisadr Parisa, Ghaffarifar Fatemeh, Mohammad Hassan Zuhair
机构信息
Department of Parasitology, School of Medical Sciences, Tarbiat Modares University, Tehran, Iran.
Department of Immunology, School of Medical Sciences, Tarbiat Modares University, Tehran, Iran.
出版信息
Iran J Pharm Res. 2013 Fall;12(4):903-9.
Artemisinin and its derivatives are very important new class of antimalarial drugs. One of the most important artemisinin derivatives is artemether. The antiparasitic activity of artemether as a derivative of artemisinin is related to endoperoxide bridge in its structure. The aim of this study was the evaluation of antileishmanial effect of artemether, with more focus on its apoptotic effect. In this study we used artemether in concentration of 5, 10, 25, 50 and 100 μg/mL for promastigote assay, promastigote proliferation measurements by MTT assay, detection of apoptotic cells by Flow cytometry analysis and DNA ladder assay. The application of artemether, promastigote IC50 was measured as 25 μg/mL. The percentage of apoptotic promastigotes by using 25 μg/mL of artemether was 42.28. The results of present study showed that artemether has inhibition effect on intracellular and extracellular growth of Leishmania major. Promastigotes of Leishmania major undergo apoptosis after exposure to artemether.
青蒿素及其衍生物是一类非常重要的新型抗疟药物。青蒿醚是最重要的青蒿素衍生物之一。青蒿醚作为青蒿素的衍生物，其抗寄生虫活性与其结构中的内过氧化物桥有关。本研究的目的是评估青蒿醚的抗利什曼原虫作用，更侧重于其凋亡作用。在本研究中，我们使用浓度为5、10、25、50和100μg/mL的青蒿醚进行前鞭毛体测定，通过MTT法测量前鞭毛体增殖，通过流式细胞术分析和DNA梯状条带分析检测凋亡细胞。应用青蒿醚时，前鞭毛体的IC50测定为25μg/mL。使用25μg/mL青蒿醚时，凋亡前鞭毛体的百分比为42.28。本研究结果表明，青蒿醚对杜氏利什曼原虫的细胞内和细胞外生长均有抑制作用。杜氏利什曼原虫的前鞭毛体在接触青蒿醚后会发生凋亡。
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