TY - JOUR
T1 - Xanthohumol is a potent pan-inhibitor of coronaviruses targeting main protease
AU - Lin, Yuxi
AU - Zang, Ruochen
AU - Ma, Yanlong
AU - Wang, Zhuoya
AU - Li, Li
AU - Ding, Siyuan
AU - Zhang, Rong
AU - Wei, Zhiqiang
AU - Yang, Jinbo
AU - Wang, Xin
N1 - Funding Information:
Acknowledgments: We acknowledge Xin, Li for providing the expression vector, pGEX4T1-Mpro. Furthermore, the authors give thanks for the financial support from Washington University (S. Louis) and Shanghai Medical College.
Funding Information:
Funding: This research was funded by the special scientific research fund for COVID-19 from the Pilot National Laboratory for Marine Science and Technology (Qingdao) (QNLM202001), the National Natural Science Foundation of China (81991525, 31700755), the Taishan Scholars Program (tsqn201909170), the Fundamental Research Funds for the Central Universities to X.W., the Innovative Leader of the Qingdao Program (19–3-2–26-zhc), and the National Natural Science Foundation of China (32041005).
Publisher Copyright:
© 2021 by the authors. Li-censee MDPI, Basel, Switzerland.
PY - 2021/11/1
Y1 - 2021/11/1
N2 - Coronaviruses cause diseases in humans and livestock. The SARS-CoV-2 is infecting mil-lions 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 attrac-tive drug target for antiviral drug development. It has been extensively discussed whether Xantho-humol 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 alphacoro-navirus 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.
AB - Coronaviruses cause diseases in humans and livestock. The SARS-CoV-2 is infecting mil-lions 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 attrac-tive drug target for antiviral drug development. It has been extensively discussed whether Xantho-humol 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 alphacoro-navirus 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.
KW - Coronavirus
KW - Natural product
KW - PEDV
KW - SARS-CoV-2
KW - Xanthohumol
UR - http://www.scopus.com/inward/record.url?scp=85118687093&partnerID=8YFLogxK
U2 - 10.3390/ijms222212134
DO - 10.3390/ijms222212134
M3 - Article
C2 - 34830015
AN - SCOPUS:85118687093
SN - 1661-6596
VL - 22
JO - International Journal of Molecular Sciences
JF - International Journal of Molecular Sciences
IS - 22
M1 - 12134
ER -