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首页> 外文期刊>The American Journal of Tropical Medicine and Hygiene >In vitro activity of artemisinin in combination with clotrimazole or heat-treated amphotericin B against Plasmodium falciparum.
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In vitro activity of artemisinin in combination with clotrimazole or heat-treated amphotericin B against Plasmodium falciparum.

机译:青蒿素联合克霉唑或经热处理的两性霉素B的体外抗恶性疟原虫活性。

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摘要

Currently available artemisinin-based combination therapies (ACTs) for malaria are inadequate. There remains an enormous unmet need for alternate artemisinin-based combination therapies. One of the fastest methods to identify promising artemisinin-based combination therapies is to look for synergistic or additive antimalarial interaction between artemisinin and an alternate drug against P. falciparum in vitro. Amphotericin B and clotrimazole are known drugs for treatment of human fungal infections. We repurposed clotrimazole or heat-treated amphotericin B in fixed ratio combination with artemisinin for antimalarial properties. Isobologram results show synergistic/additive interaction in both of the cases at therapeutically safe concentrations. Artemisinin, clotrimazole, and their synergistic combinations also decrease hemozoin production in parasitized erythrocytes. New permeation pathways induced in infected cells remain unaffected by drug combinations as indicated by sorbitol lysis. It would be interesting to extend the studies' in vivo system.
机译:目前可用的基于青蒿素的疟疾联合疗法(ACTs)不足。对于基于青蒿素的替代疗法仍然存在巨大的需求缺口。鉴定有前途的基于青蒿素的联合疗法的最快方法之一是在体外寻找青蒿素与抗恶性疟原虫的替代药物之间的协同或加成抗疟作用。两性霉素B和克霉唑是已知的用于治疗人真菌感染的药物。我们将克霉唑或经热处理的两性霉素B与青蒿素以固定比例组合用于抗疟疾。等效线图结果显示在两种情况下,在治疗安全浓度下的协同/加性相互作用。青蒿素,克霉唑及其协同组合也可减少寄生红细胞中的血红素生成。如山梨糖醇裂解所表明,在感染细胞中诱导的新渗透途径仍不受药物组合的影响。扩展研究的体内系统将是有趣的。

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