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International Journal of Molecular Sciences
Article . 2021 . Peer-reviewed
License: CC BY
Data sources: Crossref
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PubMed Central
Other literature type . 2021
License: CC BY
Data sources: PubMed Central
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Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease

Authors: Xin Wang; Zhuoya Wang; Rong Zhang; Ruochen Zang; Ruochen Zang; Jinbo Yang; Zhiqiang Wei; +4 Authors

Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease

Abstract

Coronaviruses cause diseases in humans and livestock. The SARS-CoV-2 is infecting millions of human beings, with high morbidity and mortality worldwide. The main protease (Mpro) of coronavirus plays a pivotal role in viral replication and transcription, which, in theory, is an attractive drug target for antiviral drug development. It has been extensively discussed whether Xanthohumol is able to help COVID-19 patients. Here, we report that Xanthohumol, a small molecule in clinical trials from hops (Humulus lupulus), was a potent pan-inhibitor for various coronaviruses by targeting Mpro, for example, betacoronavirus SARS-CoV-2 (IC50 value of 1.53 μM), and alphacoronavirus PEDV (IC50 value of 7.51 μM). Xanthohumol inhibited Mpro activities in the enzymatical assays, while pretreatment with Xanthohumol restricted the SARS-CoV-2 and PEDV replication in Vero-E6 cells. Therefore, Xanthohumol is a potent pan-inhibitor of coronaviruses and an excellent lead compound for further drug development.

Keywords

natural product, coronavirus, Virus Replication, Article, Catalytic Domain, Chlorocebus aethiops, Animals, Humans, Protease Inhibitors, Amino Acid Sequence, Vero Cells, Flavonoids, Biological Products, Propiophenones, Binding Sites, SARS-CoV-2, Xanthohumol, PEDV, 3C Viral Proteases, Alphacoronavirus, COVID-19, COVID-19 Drug Treatment, Coronavirus, Molecular Docking Simulation, Sequence Alignment

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    citations
    This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    28
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Top 10%
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    Average
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    Top 10%
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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
28
Top 10%
Average
Top 10%
Green
gold