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Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease.
Lin, Yuxi; Zang, Ruochen; Ma, Yanlong; Wang, Zhuoya; Li, Li; Ding, Siyuan; Zhang, Rong; Wei, Zhiqiang; Yang, Jinbo; Wang, Xin.
  • Lin Y; Institute of Cancer Biology and Drug Screening, School of Life Sciences, Lanzhou University, Lanzhou 730000, China.
  • Zang R; Center for Innovation Marine Drug Screening and Evaluation, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China.
  • Ma Y; Department of Molecular Microbiology, School of Medicine, Washington University, St. Louis, MO 63110, USA.
  • Wang Z; Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
  • Li L; Key Laboratory of Medical Molecular Virology (MOE/NHC/CAMS), Shanghai Institute of Infectious Disease and Biosecurity, School of Basic Medical Sciences, Shanghai Medical College, Fudan University, Shanghai 200032, China.
  • Ding S; Center for High Performance Computing and System Simulation, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China.
  • Zhang R; Center for Innovation Marine Drug Screening and Evaluation, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China.
  • Wei Z; Department of Molecular Microbiology, School of Medicine, Washington University, St. Louis, MO 63110, USA.
  • Yang J; Key Laboratory of Medical Molecular Virology (MOE/NHC/CAMS), Shanghai Institute of Infectious Disease and Biosecurity, School of Basic Medical Sciences, Shanghai Medical College, Fudan University, Shanghai 200032, China.
  • Wang X; Center for High Performance Computing and System Simulation, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China.
Int J Mol Sci ; 22(22)2021 Nov 09.
Article in English | MEDLINE | ID: covidwho-1512384
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 (Mpro) 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 Mpro, for example, betacoronavirus SARS-CoV-2 (IC50 value of 1.53 µM), and alphacoronavirus 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.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Propiophenones / Protease Inhibitors / Flavonoids / 3C Viral Proteases / SARS-CoV-2 Type of study: Prognostic study Language: English Year: 2021 Document Type: Article Affiliation country: Ijms222212134

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Propiophenones / Protease Inhibitors / Flavonoids / 3C Viral Proteases / SARS-CoV-2 Type of study: Prognostic study Language: English Year: 2021 Document Type: Article Affiliation country: Ijms222212134