抗疟药物：它们对疟原虫配子体的有效性如何？
Anti-malarial drugs: how effective are they against Plasmodium falciparum gametocytes?
机构信息
Malaria Biology Laboratory, Queensland Institute of Medical Research, 300 Herston Rd, Herston 4006, Queensland, Australia.
出版信息
Malar J. 2012 Feb 6;11:34. doi: 10.1186/1475-2875-11-34.
BACKGROUND
Recent renewed emphasis on the eradication of malaria has highlighted the need for more tools with which to achieve this ambitious goal. One high priority area is the need to determine the gametocytocidal activity of both currently used anti-malarial drugs and those in the development pipeline. However, testing the activity of compounds against Plasmodium falciparum gametocytes is technically challenging both in vivo and in vitro.
METHODS
Here the use of a simple robust assay to screen a panel of currently used and experimental anti-malarial drugs against mature P. falciparum gametocytes is described.
RESULTS
Eight of 44 compounds tested reduced gametocyte viability by at least 50% and three showed IC50 values in nM range.
CONCLUSIONS
There is a need to identify new compounds with activity against late stage gametocytes and the information provided by this in vitro assay is a valuable first step, which can guide future clinical studies.
背景
最近重新强调消除疟疾，这凸显了我们需要更多的工具来实现这一雄心勃勃的目标。一个高度优先的领域是需要确定目前使用的抗疟药物和处于开发管道中的药物的配子体杀灭活性。然而，在体内和体外检测化合物对恶性疟原虫配子体的活性都是具有技术挑战性的。
方法
本文描述了一种简单而稳健的检测方法，用于筛选一组目前使用的和实验性的抗疟药物对成熟恶性疟原虫配子体的作用。
结果
在测试的 44 种化合物中有 8 种使配子体活力至少降低了 50%，有 3 种化合物的 IC50 值在纳摩尔范围内。
结论
有必要确定具有晚期配子体活性的新化合物，而该体外检测提供的信息是一个有价值的第一步，可以指导未来的临床研究。
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