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 - 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 -