植物来源的 SARS-CoV-2 病毒进入抑制剂：一种系统发育学视角。

Botanical inhibitors of SARS-CoV-2 viral entry: a phylogenetic perspective.

机构信息

Molecular and Systems Pharmacology, Laney Graduate School, Emory University, Atlanta, GA, USA.

Center for the Study of Human Health, Emory University, Atlanta, GA, USA.

出版信息

Sci Rep. 2023 Jan 23;13(1):1244. doi: 10.1038/s41598-023-28303-x.

DOI:10.1038/s41598-023-28303-x

PMID:36690683

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9868516/

Abstract

Throughout the SARS-CoV-2 pandemic, the use of botanical dietary supplements in the United States has increased, yet their safety and efficacy against COVID-19 remains underexplored. The Quave Natural Product Library is a phylogenetically diverse collection of botanical and fungal natural product extracts including popular supplement ingredients. Evaluation of 1867 extracts and 18 compounds for virus spike protein binding to host cell ACE2 receptors in a SARS-CoV-2 pseudotyped virus system identified 310 extracts derived from 188 species across 76 families (3 fungi, 73 plants) that exhibited ≥ 50% viral entry inhibition activity at 20 µg/mL. Extracts exhibiting mammalian cytotoxicity > 15% and those containing cardiotoxic cardiac glycosides were eliminated. Three extracts were selected for further testing against four pseudotyped variants and infectious SARS-CoV-2 and were then further chemically characterized, revealing the potent (EC < 5 µg/mL) antiviral activity of Solidago altissima L. (Asteraceae) flowers and Pteridium aquilinum (L.) Kuhn (Dennstaedtiaceae) rhizomes.

摘要

在整个 SARS-CoV-2 大流行期间，美国植物性膳食补充剂的使用有所增加，但它们在预防 COVID-19 方面的安全性和有效性仍未得到充分探索。Quave 天然产物文库是一个具有系统发育多样性的植物和真菌天然产物提取物的集合，其中包括流行的补充剂成分。在 SARS-CoV-2 假病毒系统中评估了 1867 种提取物和 18 种化合物对病毒刺突蛋白与宿主细胞 ACE2 受体的结合，发现 310 种提取物来自 76 个科的 188 种植物（3 种真菌，73 种植物），在 20 µg/mL 时表现出 ≥50%的病毒进入抑制活性。对哺乳动物细胞毒性 >15%的提取物和含有心脏毒性强心苷的提取物被排除在外。选择了三种提取物进一步针对四种假型变体和传染性 SARS-CoV-2 进行测试，然后进一步进行化学表征，揭示了 Solidago altissima L.（菊科）花和 Pteridium aquilinum（L.）Kuhn（水龙骨科）根茎的强大（EC <5 µg/mL）抗病毒活性。