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他普司他汀:新型靶向宿主冠状病毒抗病毒药物的关键?

Thapsigargin: key to new host-directed coronavirus antivirals?

机构信息

Rudolf Buchheim Institute of Pharmacology, Justus Liebig University, Giessen, Germany.

Institute of Biochemistry, Justus Liebig University, Giessen, Germany; German Center for Lung Research (DZL) and Universities of Giessen and Marburg Lung Center (UGMLC), Giessen, Germany.

出版信息

Trends Pharmacol Sci. 2022 Jul;43(7):557-568. doi: 10.1016/j.tips.2022.04.004. Epub 2022 Apr 18.

DOI:10.1016/j.tips.2022.04.004
PMID:35534355
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9013669/
Abstract

Despite the great success of vaccines that protect against RNA virus infections, and the development and clinical use of a limited number of RNA virus-specific drugs, there is still an urgent need for new classes of antiviral drugs against circulating or emerging RNA viruses. To date, it has proved difficult to efficiently suppress RNA virus replication by targeting host cell functions, and there are no approved drugs of this type. This opinion article discusses the recent discovery of a pronounced and sustained antiviral activity of the plant-derived natural compound thapsigargin against enveloped RNA viruses such as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), Middle East respiratory syndrome coronavirus (MERS-CoV), and influenza A virus. Based on its mechanisms of action, thapsigargin represents a new prototype of compounds with multimodal host-directed antiviral activity.

摘要

尽管针对 RNA 病毒感染的疫苗取得了巨大成功,并且开发并临床应用了少数几种针对 RNA 病毒的特异性药物,但仍然迫切需要针对循环或新出现的 RNA 病毒的新型抗病毒药物。迄今为止,通过靶向宿主细胞功能来有效抑制 RNA 病毒复制已被证明非常困难,并且尚无此类批准的药物。本文讨论了从植物中提取的天然化合物 thapsigargin 对包膜 RNA 病毒(如严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)、中东呼吸综合征冠状病毒(MERS-CoV)和甲型流感病毒)具有显著且持久的抗病毒活性的最新发现。基于其作用机制,thapsigargin 代表了具有多模式宿主导向抗病毒活性的新型化合物原型。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e4e2/9013669/947e3fa41343/gr2_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e4e2/9013669/69a3b7fab29a/gr1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e4e2/9013669/de1e84b0a314/b1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e4e2/9013669/947e3fa41343/gr2_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e4e2/9013669/69a3b7fab29a/gr1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e4e2/9013669/de1e84b0a314/b1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e4e2/9013669/947e3fa41343/gr2_lrg.jpg

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本文引用的文献

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Molecules. 2021 Dec 9;26(24):7469. doi: 10.3390/molecules26247469.
2
Emergent SARS-CoV-2 variants: comparative replication dynamics and high sensitivity to thapsigargin.紧急出现的 SARS-CoV-2 变体:复制动力学的比较和对他普司他汀的高敏感性。
Virulence. 2021 Dec;12(1):2946-2956. doi: 10.1080/21505594.2021.2006960.
3
Using soft X-ray tomography for rapid whole-cell quantitative imaging of SARS-CoV-2-infected cells.
J Dent Res. 2025 Jun;104(6):656-667. doi: 10.1177/00220345241307944. Epub 2025 Feb 4.
4
Preclinical and Clinical Investigations of Potential Drugs and Vaccines for COVID-19 Therapy: A Comprehensive Review With Recent Update.COVID-19治疗潜在药物和疫苗的临床前与临床研究:近期更新的综合综述
Clin Pathol. 2024 Jul 26;17:2632010X241263054. doi: 10.1177/2632010X241263054. eCollection 2024 Jan-Dec.
5
Plants as Biofactories for Therapeutic Proteins and Antiviral Compounds to Combat COVID-19.植物作为生产治疗性蛋白质和抗病毒化合物以对抗新冠病毒的生物工厂。
Life (Basel). 2023 Feb 23;13(3):617. doi: 10.3390/life13030617.
6
The Role of Cyclodextrins in COVID-19 Therapy-A Literature Review.环糊精在 COVID-19 治疗中的作用——文献综述。
Int J Mol Sci. 2023 Feb 3;24(3):2974. doi: 10.3390/ijms24032974.
7
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Viruses. 2023 Jan 4;15(1):156. doi: 10.3390/v15010156.
8
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Nat Commun. 2021 Feb 11;12(1):961. doi: 10.1038/s41467-021-21213-4.