Xanthohumol is a potent pan-inhibitor of coronaviruses targeting main protease

Yuxi Lin, Ruochen Zang, Yanlong Ma, Zhuoya Wang, Li Li, Siyuan Ding, Rong Zhang, Zhiqiang Wei, Jinbo Yang, Xin Wang

Research output: Contribution to journalArticlepeer-review

4 Scopus citations

Abstract

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.

Original languageEnglish
Article number12134
JournalInternational journal of molecular sciences
Volume22
Issue number22
DOIs
StatePublished - Nov 1 2021

Keywords

  • Coronavirus
  • Natural product
  • PEDV
  • SARS-CoV-2
  • Xanthohumol

Fingerprint

Dive into the research topics of 'Xanthohumol is a potent pan-inhibitor of coronaviruses targeting main protease'. Together they form a unique fingerprint.

Cite this