PMID: Int J Mol Sci. 2021 Nov 9 ;22(22). Epub 2021 Nov 9. PMID: 34830015 Abstract Title: 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 (M) 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 (), was a potent pan-inhibitor for various coronaviruses by targeting M, for example, betacoronavirus SARS-CoV-2 (ICvalue of 1.53μM), and alphacoronavirus PEDV (ICvalue of 7.51μM). Xanthohumol inhibited Mactivities 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.
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