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  • 标题:Real-time and automated monitoring of antischistosomal drug activity profiles for screening of compound libraries
  • 本地全文:下载
  • 作者:Paolo S. Ravaynia ; Stefan Biendl ; Francesco Grassi
  • 期刊名称:iScience
  • 印刷版ISSN:2589-0042
  • 出版年度:2022
  • 卷号:25
  • 期号:4
  • 页码:1-20
  • DOI:10.1016/j.isci.2022.104087
  • 语种:English
  • 出版社:Elsevier
  • 摘要:SummarySchistosomiasis is a neglected tropical disease that affects over 200 million people annually. As the antischistosomal drug pipeline is currently empty, repurposing of compound libraries has become a source for accelerating drug development, which demands the implementation of high-throughput and efficient screening strategies. Here, we present a parallelized impedance-based platform for continuous and automated viability evaluation ofSchistosoma mansonischistosomula in 128 microwells during 72 h to identify antischistosomal hitsin vitro. By initially screening 57 repurposed compounds against larvae, five drugs are identified, which reduce parasite viability by more than 70%. The activity profiles of the selected drugs are then investigated via real-time dose-response monitoring, and four compounds reveal high potency and rapid action, which renders them suitable candidates for follow-up tests against adult parasites. The study shows that our device is a reliable tool for real-time drug screening analysis of libraries to identify new promising therapeutics against schistosomiasis.Graphical abstractDisplay OmittedHighlights•Scalable, plastic microwell chip with integrated platinum electrodes•Automated impedance-based recording of 128 microwell units in parallel•Continuous monitoring ofin vitrodrug library efficacy on schistosomula for 72 h•Identification of four fast-acting antischistosomal drugs forin vivotestingBiotechnology; Drugs; Microbiology parasite; Monitoring feature; Signal processing
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