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

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...

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Autores principales:	Yuyong Zhou, Kerry Gilmore, Santseharay Ramirez, Eva Settels, Karen A. Gammeltoft, Long V. Pham, Ulrik Fahnøe, Shan Feng, Anna Offersgaard, Jakob Trimpert, Jens Bukh, Klaus Osterrieder, Judith M. Gottwein, Peter H. Seeberger
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/cb60e70748c8410cbc59a6f8b48eb14d
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spelling	oai:doaj.org-article:cb60e70748c8410cbc59a6f8b48eb14d2021-12-02T15:33:13ZIn vitro efficacy of artemisinin-based treatments against SARS-CoV-210.1038/s41598-021-93361-y2045-2322https://doaj.org/article/cb60e70748c8410cbc59a6f8b48eb14d2021-07-01T00:00:00Zhttps://doi.org/10.1038/s41598-021-93361-yhttps://doaj.org/toc/2045-2322Abstract 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.Yuyong ZhouKerry GilmoreSantseharay RamirezEva SettelsKaren A. GammeltoftLong V. PhamUlrik FahnøeShan FengAnna OffersgaardJakob TrimpertJens BukhKlaus OsterriederJudith M. GottweinPeter H. SeebergerNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 11, Iss 1, Pp 1-14 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Yuyong Zhou Kerry Gilmore Santseharay Ramirez Eva Settels Karen A. Gammeltoft Long V. Pham Ulrik Fahnøe Shan Feng Anna Offersgaard Jakob Trimpert Jens Bukh Klaus Osterrieder Judith M. Gottwein Peter H. Seeberger In vitro efficacy of artemisinin-based treatments against SARS-CoV-2
description	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.
format	article
author	Yuyong Zhou Kerry Gilmore Santseharay Ramirez Eva Settels Karen A. Gammeltoft Long V. Pham Ulrik Fahnøe Shan Feng Anna Offersgaard Jakob Trimpert Jens Bukh Klaus Osterrieder Judith M. Gottwein Peter H. Seeberger
author_facet	Yuyong Zhou Kerry Gilmore Santseharay Ramirez Eva Settels Karen A. Gammeltoft Long V. Pham Ulrik Fahnøe Shan Feng Anna Offersgaard Jakob Trimpert Jens Bukh Klaus Osterrieder Judith M. Gottwein Peter H. Seeberger
author_sort	Yuyong Zhou
title	In vitro efficacy of artemisinin-based treatments against SARS-CoV-2
title_short	In vitro efficacy of artemisinin-based treatments against SARS-CoV-2
title_full	In vitro efficacy of artemisinin-based treatments against SARS-CoV-2
title_fullStr	In vitro efficacy of artemisinin-based treatments against SARS-CoV-2
title_full_unstemmed	In vitro efficacy of artemisinin-based treatments against SARS-CoV-2
title_sort	in vitro efficacy of artemisinin-based treatments against sars-cov-2
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/cb60e70748c8410cbc59a6f8b48eb14d
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In vitro efficacy of artemisinin-based treatments against SARS-CoV-2

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