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用于治疗恰加斯病的植物资源中的系统生物活性热点。

Phylobioactive hotspots in plant resources used to treat Chagas disease.

作者信息

Salm Andrea, Krishnan Sandhya R, Collu Marta, Danton Ombeline, Hamburger Matthias, Leonti Marco, Almanza Giovanna, Gertsch Jürg

机构信息

Institute of Biochemistry and Molecular Medicine, University of Bern, Bern, Switzerland.

Department of Biomedical Sciences, University of Cagliari, Cagliari, Italy.

出版信息

iScience. 2021 Mar 15;24(4):102310. doi: 10.1016/j.isci.2021.102310. eCollection 2021 Apr 23.

DOI:10.1016/j.isci.2021.102310
PMID:33870129
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8040286/
Abstract

Globally, more than six million people are infected with , 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 Mediterranean a 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 of , the taxon with the strongest ethnomedical consensus for treating CD among the Izoceño-Guaraní. Testing common 9,10-anthracenedione derivatives in cellular infection assays demarcates hydroxyanthraquinone as a potential antichagasic lead scaffold. Our study systematically uncovers antichagasic phylogenetic hotspots in the plant kingdom as a potential resource for drug discovery based on ethnopharmacological hypotheses.

摘要

在全球范围内,超过600万人感染了克氏锥虫,它是媒介传播的恰加斯病(CD)的致病原生动物寄生虫。我们在玻利维亚不同民族中开展了一项横断面民族药理学实地研究,这些民族所在地区恰加斯病高度流行。在一项多维分析中,对玻利维亚用于治疗恰加斯病的775种植物药提取物以及两千年前由狄奥斯科里季斯汇编的来自地中海地区、用于无关适应症的植物药进行了分析,发现了不同的抗恰加斯病天然产物类别。有趣的是,植物生物活性蒽醌热点与伊佐塞诺-瓜拉尼人中治疗恰加斯病民族医学共识最强的分类群——的抗恰加斯病活性相匹配。在细胞感染试验中测试常见的9,10-蒽二酮衍生物,确定羟基蒽醌为一种潜在的抗恰加斯病先导支架。我们的研究基于民族药理学假设,系统地揭示了植物界中的抗恰加斯病系统发生热点,作为药物发现的潜在资源。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/c122c3b389ea/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/74928a8d9c50/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/9b3ea685875a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/72f5242fbb98/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/0a009f64fe38/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/71d6fde57905/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/7684aa061c2b/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/3f3e09d847fb/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/c122c3b389ea/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/74928a8d9c50/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/9b3ea685875a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/72f5242fbb98/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/0a009f64fe38/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/71d6fde57905/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/7684aa061c2b/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/3f3e09d847fb/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b048/8040286/c122c3b389ea/gr7.jpg

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