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DOI	10.1073/pnas.2021579118
	Identification of existing pharmaceuticals and herbal medicines as inhibitors of SARS-CoV-2 infection
	Jan J.-T.; Cheng T.-J.R.; Juang Y.-P.; Ma H.-H.; Wu Y.-T.; Yang W.-B.; Cheng C.-W.; Chen X.; Chou T.-H.; Shie J.-J.; Cheng W.-C.; Chein R.-J.; Mao S.-S.; Liang P.-H.; Ma C.; Hung S.-C.; Wong C.-H.
发表日期	2021
ISSN	00278424
卷号	118 期号:5
英文摘要	The outbreak of COVID-19 caused by SARS-CoV-2 has resulted in more than 50 million confirmed cases and over 1 million deaths worldwide as of November 2020. Currently, there are no effective antivirals approved by the Food and Drug Administration to contain this pandemic except the antiviral agent remdesivir. In addition, the trimeric spike protein on the viral surface is highly glycosylated and almost 200,000 variants with mutations at more than 1,000 positions in its 1,273 amino acid sequence were reported, posing a major challenge in the development of antibodies and vaccines. It is therefore urgently needed to have alternative and timely treatments for the disease. In this study, we used a cell-based infection assay to screen more than 3,000 agents used in humans and animals, including 2,855 small molecules and 190 traditional herbal medicines, and identified 15 active small molecules in concentrations ranging from 0.1 nM to 50 μM. Two enzymatic assays, along with molecular modeling, were then developed to confirm those targeting the virus 3CL protease and the RNA-dependent RNA polymerase. Several water extracts of herbal medicines were active in the cell-based assay and could be further developed as plant-derived anti–SARS-CoV-2 agents. Some of the active compounds identified in the screen were further tested in vivo, and it was found that mefloquine, nelfinavir, and extracts of Ganoderma lucidum (RF3), Perilla frutescens, and Mentha haplocalyx were effective in a challenge study using hamsters as disease model. © 2021 National Academy of Sciences. All rights reserved.
英文关键词	Animal studies; Antiviral; Cell-based; Drug repurposing; SARS-CoV-2
语种	英语
scopus关键词	antivirus agent; plant extract; adult; animal; chemistry; Chlorocebus aethiops; disease model; drug effect; drug repositioning; drug therapy; epidemiology; female; genetics; hamster; human; male; pandemic; procedures; Vero cell line; virology; Adult; Animals; Antiviral Agents; Chlorocebus aethiops; COVID-19; Cricetinae; Disease Models, Animal; Drug Repositioning; Female; Humans; Male; Pandemics; Plant Extracts; SARS-CoV-2; Vero Cells
来源期刊	Proceedings of the National Academy of Sciences of the United States of America
文献类型	期刊论文
条目标识符	http://gcip.llas.ac.cn/handle/2XKMVOVA/180809
作者单位	Genomics Research Center, Academia Sinica, Taipei, 115, Taiwan; School of Pharmacy, National Taiwan University, Taipei, 110, Taiwan; Institute of Chemistry, Academia Sinica, Taipei, 128, Taiwan; Department of Chemistry, Scripps Research Institute, San diego, CA 92037, United States
推荐引用方式 GB/T 7714	Jan J.-T.,Cheng T.-J.R.,Juang Y.-P.,et al. Identification of existing pharmaceuticals and herbal medicines as inhibitors of SARS-CoV-2 infection[J],2021,118(5).
APA	Jan J.-T..,Cheng T.-J.R..,Juang Y.-P..,Ma H.-H..,Wu Y.-T..,...&Wong C.-H..(2021).Identification of existing pharmaceuticals and herbal medicines as inhibitors of SARS-CoV-2 infection.Proceedings of the National Academy of Sciences of the United States of America,118(5).
MLA	Jan J.-T.,et al."Identification of existing pharmaceuticals and herbal medicines as inhibitors of SARS-CoV-2 infection".Proceedings of the National Academy of Sciences of the United States of America 118.5(2021).