Center for Neglected Diseases Drug Discovery (CND3), Institut Pasteur Korea, Seongnam-si, Gyeonggi-do, South Korea.
PLoS One. 2012;7(8):e41765. doi: 10.1371/journal.pone.0041765. Epub 2012 Aug 29.
Placental malaria is a significant cause of all malaria-related deaths globally for which no drugs have been developed to specifically disrupt its pathogenesis. To facilitate the discovery of antimalarial drugs targeting the cytoadherence process of Plasmodium-infected erythrocytes in the placenta microvasculature, we have developed an automated image-based assay for high-throughput screening for potent cytoadherence inhibitors in vitro. Parasitized erythrocytes were drug-treated for 24 h and then allowed to adhere on a monolayer of placental BeWo cells prior to red blood cell staining with glycophorin A antibodies. Upon image-acquisition, drug effects were quantified as the proportion of treated parasitized erythrocytes to BeWo cells compared to the binding of untreated iRBCs. We confirmed the reliability of this new assay by comparing the binding ratios of CSA- and CD36-panned parasites on the placental BeWo cells, and by quantifying the effects of chondroitin sulfate A, brefeldin A, and artemisinin on the binding. By simultaneously examining the drug effects on parasite viability, we could discriminate between cytoadherence-specific inhibitors and other schizonticidal compounds. Taken together, our data establish that the developed assay is highly suitable for drug studies targeting placental malaria, and will facilitate the discovery and rapid development of new therapies against malaria.
胎盘疟疾是全球所有与疟疾相关死亡的重要原因,但目前尚无专门用于破坏其发病机制的药物。为了促进针对胎盘微血管中感染疟原虫的红细胞细胞黏附过程的抗疟药物的发现,我们开发了一种自动化的基于图像的体外高通量筛选强力细胞黏附抑制剂的方法。用药物处理感染疟原虫的红细胞 24 小时,然后让它们在胎盘 BeWo 细胞单层上黏附,然后用糖蛋白 A 抗体对红细胞进行染色。在采集图像后,通过比较处理过的感染红细胞与未处理的 iRBC 结合到 BeWo 细胞的比例来量化药物的作用。我们通过比较胎盘 BeWo 细胞上 CSA 和 CD36 筛选的寄生虫的结合比率,以及定量硫酸软骨素 A、布雷菲德菌素 A 和青蒿素对结合的影响,证实了这种新方法的可靠性。通过同时检查药物对寄生虫活力的影响,我们可以区分细胞黏附特异性抑制剂和其他裂殖体杀伤化合物。总之,我们的数据表明,开发的方法非常适合针对胎盘疟疾的药物研究,并将促进针对疟疾的新疗法的发现和快速发展。