Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease
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 (M<sup>pro</sup>) of coronavirus plays a pivotal role in viral replication and transcription, which, in theory, is an...
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2021
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oai:doaj.org-article:da701b4e744d46c897ce86e4a6d134bb2021-11-25T17:53:41ZXanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease10.3390/ijms2222121341422-00671661-6596https://doaj.org/article/da701b4e744d46c897ce86e4a6d134bb2021-11-01T00:00:00Zhttps://www.mdpi.com/1422-0067/22/22/12134https://doaj.org/toc/1661-6596https://doaj.org/toc/1422-0067Coronaviruses 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 (M<sup>pro</sup>) 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 (<i>Humulus lupulus</i>), was a potent pan-inhibitor for various coronaviruses by targeting M<sup>pro</sup>, for example, betacoronavirus SARS-CoV-2 (IC<sub>50</sub> value of 1.53 μM), and alphacoronavirus PEDV (IC<sub>50</sub> value of 7.51 μM). Xanthohumol inhibited M<sup>pro</sup> 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.Yuxi LinRuochen ZangYanlong MaZhuoya WangLi LiSiyuan DingRong ZhangZhiqiang WeiJinbo YangXin WangMDPI AGarticleXanthohumolnatural productSARS-CoV-2PEDVcoronavirusBiology (General)QH301-705.5ChemistryQD1-999ENInternational Journal of Molecular Sciences, Vol 22, Iss 12134, p 12134 (2021) |
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Xanthohumol natural product SARS-CoV-2 PEDV coronavirus Biology (General) QH301-705.5 Chemistry QD1-999 |
| spellingShingle |
Xanthohumol natural product SARS-CoV-2 PEDV coronavirus Biology (General) QH301-705.5 Chemistry QD1-999 Yuxi Lin Ruochen Zang Yanlong Ma Zhuoya Wang Li Li Siyuan Ding Rong Zhang Zhiqiang Wei Jinbo Yang Xin Wang Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease |
| description |
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 (M<sup>pro</sup>) 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 (<i>Humulus lupulus</i>), was a potent pan-inhibitor for various coronaviruses by targeting M<sup>pro</sup>, for example, betacoronavirus SARS-CoV-2 (IC<sub>50</sub> value of 1.53 μM), and alphacoronavirus PEDV (IC<sub>50</sub> value of 7.51 μM). Xanthohumol inhibited M<sup>pro</sup> 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. |
| format |
article |
| author |
Yuxi Lin Ruochen Zang Yanlong Ma Zhuoya Wang Li Li Siyuan Ding Rong Zhang Zhiqiang Wei Jinbo Yang Xin Wang |
| author_facet |
Yuxi Lin Ruochen Zang Yanlong Ma Zhuoya Wang Li Li Siyuan Ding Rong Zhang Zhiqiang Wei Jinbo Yang Xin Wang |
| author_sort |
Yuxi Lin |
| title |
Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease |
| title_short |
Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease |
| title_full |
Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease |
| title_fullStr |
Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease |
| title_full_unstemmed |
Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease |
| title_sort |
xanthohumol is a potent pan-inhibitor of coronaviruses targeting main protease |
| publisher |
MDPI AG |
| publishDate |
2021 |
| url |
https://doaj.org/article/da701b4e744d46c897ce86e4a6d134bb |
| work_keys_str_mv |
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| _version_ |
1718411891990069248 |