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从 L. 中分离得到的木樨草素是人类冠状病毒 229E 的潜在治疗药物。

Luteolin Isolated from L., a Potential Remedy for Human Coronavirus 229E.

机构信息

Joint Research Unit 1158, BioEcoAgro, Univ. Lille, INRAE, Univ. Liège, UPJV, JUNIA, Univ. Artois, Univ. Littoral Côte d'Opale, ICV-Institut Charles Viollette, 59650 Villeneuve-d'Ascq, France.

Laboratory of Aromatic and Medicinal Plants, Biotechnology Centre of Borj-Cedria (CBBC), Hammam-Lif 2050, Tunisia.

出版信息

Molecules. 2023 May 23;28(11):4263. doi: 10.3390/molecules28114263.

DOI:10.3390/molecules28114263
PMID:37298740
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10254368/
Abstract

The COVID-19 pandemic, caused by SARS-CoV-2, addressed the lack of specific antiviral drugs against coronaviruses. In this study, bioguided fractionation performed on both ethyl acetate and aqueous sub-extracts of stems led to identifying luteolin as a highly active antiviral molecule against human coronavirus HCoV-229E. The apolar sub-extract (CHCl) containing phenanthrene derivatives did not show antiviral activity against this coronavirus. Infection tests on Huh-7 cells, expressing or not the cellular protease TMPRSS2, using luciferase reporter virus HCoV-229E-Luc showed that luteolin exhibited a dose-dependent inhibition of infection. Respective IC values of 1.77 µM and 1.95 µM were determined. Under its glycosylated form (luteolin-7--glucoside), luteolin was inactive against HCoV-229E. Time of addition assay showed that utmost anti-HCoV-229E activity of luteolin was achieved when added at the post-inoculation step, indicating that luteolin acts as an inhibitor of the replication step of HCoV-229E. Unfortunately, no obvious antiviral activity for luteolin was found against SARS-CoV-2 and MERS-CoV in this study. In conclusion, luteolin isolated from is a new inhibitor of alphacoronavirus HCoV-229E.

摘要

由 SARS-CoV-2 引起的 COVID-19 大流行，解决了针对冠状病毒缺乏特异性抗病毒药物的问题。在这项研究中，对茎的乙酸乙酯和水亚提取物进行生物导向分离，鉴定出木犀草素是一种针对人冠状病毒 HCoV-229E 的高度活性抗病毒分子。含有菲衍生物的非极性亚提取物（CHCl）对这种冠状病毒没有抗病毒活性。使用 HCoV-229E-Luc 荧光素酶报告病毒在表达或不表达细胞蛋白酶 TMPRSS2 的 Huh-7 细胞上进行感染测试，结果表明木犀草素对感染表现出剂量依赖性抑制。分别确定了 1.77 µM 和 1.95 µM 的 IC 值。在其糖基化形式（木犀草素-7--葡萄糖苷）下，木犀草素对 HCoV-229E 无活性。添加时间测定表明，木犀草素对 HCoV-229E 的最大抗活性是在接种后添加时实现的，表明木犀草素作为 HCoV-229E 复制步骤的抑制剂发挥作用。不幸的是，在这项研究中，木犀草素对 SARS-CoV-2 和 MERS-CoV 没有明显的抗病毒活性。总之，从 中分离出的木犀草素是一种新型的α冠状病毒 HCoV-229E 抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eaba/10254368/00c788c9507a/molecules-28-04263-g012.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eaba/10254368/084e4248e5ea/molecules-28-04263-g008.jpg
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