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标题：Phylobioactive hotspots in plant resources used to treat Chagas disease
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作者：Andrea Salm ; Sandhya R. Krishnan ; Marta Collu 等
期刊名称：iScience
印刷版ISSN：2589-0042
出版年度：2021
卷号：24
期号：4
页码：1-39
DOI：10.1016/j.isci.2021.102310
语种：English
出版社：Elsevier
摘要：SummaryGlobally, more than six million people are infected withTrypanosoma cruzi, the causative protozoan parasite of the vector-borne Chagas disease (CD). We conducted a cross-sectional ethnopharmacological field study in Bolivia among different ethnic groups where CD is hyperendemic. A total of 775 extracts of botanical drugs used in Bolivia in the context of CD and botanical drugs from unrelated indications from the MediterraneanDe Materia Medica compiled by Dioscorides two thousand years ago were profiled in a multidimensional assay uncovering different antichagasic natural product classes. Intriguingly, the phylobioactive anthraquinone hotspot matched the antichagasic activity ofSenna chloroclada, the taxon with the strongest ethnomedical consensus for treating CD among the Izoceño-Guaraní. Testing common 9,10-anthracenedione derivatives inT. cruzicellular infection assays demarcates hydroxyanthraquinone as a potential antichagasic lead scaffold. Our study systematically uncoversin vitroantichagasic phylogenetic hotspots in the plant kingdom as a potential resource for drug discovery based on ethnopharmacological hypotheses.Graphical abstractDisplay OmittedHighlights•Ethnopharmacological fieldwork on antichagasic medicinal plants in Bolivia•Bioprospecting of natural product classes effective againstTrypanosoma cruzi•Isolation of natural products able to inhibitT. cruzihost cell infection•Structure-activity relationship study on the antichagasic effects of anthraquinonesNatural Product Chemistry; Ethnopharmacology; Biological Sciences; Plant Biology; Plants; Bioactive Plant Product; Ethnobotany