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  In vitro efficacy of artemisinin-based treatments against SARS-CoV-2

Zhou, Y., Gilmore, K., Ramirez, S., Settels, E., Gammeltoft, K. A., Pham, L. V., et al. (2021). In vitro efficacy of artemisinin-based treatments against SARS-CoV-2. Scientific Reports, 11: 14571. doi:10.1038/s41598-021-93361-y.

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 Creators:
Zhou, Yuyong, Author
Gilmore, Kerry1, Author              
Ramirez, Santseharay, Author
Settels, Eva2, Author              
Gammeltoft, Karen A., Author
Pham, Long V., Author
Fahnøe, Ulrik, Author
Feng, Shan, Author
Offersgaard, Anna, Author
Trimpert, Jakob, Author
Bukh, Jens, Author
Osterrieder, Klaus, Author
Gottwein, Judith M., Author
Seeberger, Peter H.3, Author              
Affiliations:
1Kerry Gilmore, Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society, ou_1863304              
2Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society, ou_1863286              
3Peter H. Seeberger - Automated Systems, Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society, ou_1863306              

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Free keywords: drug discovery, viral infection
 Abstract: Effective and affordable treatments for patients suffering from coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), are needed. We report in vitro efficacy of Artemisia annua extracts as well as artemisinin, artesunate, and artemether against SARS-CoV-2. The latter two are approved active pharmaceutical ingredients of anti-malarial drugs. Concentration–response antiviral treatment assays, based on immunostaining of SARS-CoV-2 spike glycoprotein, revealed that treatment with all studied extracts and compounds inhibited SARS-CoV-2 infection of VeroE6 cells, human hepatoma Huh7.5 cells and human lung cancer A549-hACE2 cells, without obvious influence of the cell type on antiviral efficacy. In treatment assays, artesunate proved most potent (range of 50% effective concentrations (EC50) in different cell types: 7–12 µg/mL), followed by artemether (53–98 µg/mL), A. annua extracts (83–260 µg/mL) and artemisinin (151 to at least 208 µg/mL). The selectivity indices (SI), calculated based on treatment and cell viability assays, were mostly below 10 (range 2 to 54), suggesting a small therapeutic window. Time-of-addition experiments in A549-hACE2 cells revealed that artesunate targeted SARS-CoV-2 at the post-entry level. Peak plasma concentrations of artesunate exceeding EC50 values can be achieved. Clinical studies are required to further evaluate the utility of these compounds as COVID-19 treatment.

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Language(s): eng - English
 Dates: 2021-07-162021
 Publication Status: Published in print
 Pages: -
 Publishing info: -
 Table of Contents: -
 Rev. Type: -
 Identifiers: DOI: 10.1038/s41598-021-93361-y
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Title: Scientific Reports
  Abbreviation : Sci. Rep.
Source Genre: Journal
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Publ. Info: London, UK : Nature Publishing Group
Pages: 14571 Volume / Issue: 11 Sequence Number: 14571 Start / End Page: - Identifier: ISSN: 2045-2322