Journal
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Volume 22, Issue 22, Pages -Publisher
MDPI
DOI: 10.3390/ijms222212134
Keywords
Xanthohumol; natural product; SARS-CoV-2; PEDV; coronavirus
Funding
- Pilot National Laboratory for Marine Science and Technology (Qingdao) [QNLM202001]
- National Natural Science Foundation of China [81991525, 31700755, 32041005]
- Taishan Scholars Program [tsqn201909170]
- Fundamental Research Funds for the Central Universities
- Innovative Leader of the Qingdao Program [19-3-2-26-zhc]
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Xanthohumol, a small molecule from hops, has shown potent inhibitory effects against various coronaviruses by targeting M-pro, making it a promising antiviral drug candidate.
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-pro) 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 M-pro, for example, betacoronavirus SARS-CoV-2 (IC50 value of 1.53 mu M), and alphacoronavirus PEDV (IC50 value of 7.51 mu M). Xanthohumol inhibited M-pro 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.
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