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Media type:
E-Article
Title:
In vitro efficacy of artemisinin-based treatments against SARS-CoV-2
Contributor:
Zhou, Yuyong;
Gilmore, Kerry;
Ramirez, Santseharay;
Settels, Eva;
Gammeltoft, Karen A.;
Pham, Long V.;
Fahnøe, Ulrik;
Feng, Shan;
Offersgaard, Anna;
Trimpert, Jakob;
Bukh, Jens;
Osterrieder, Klaus;
Gottwein, Judith M.;
Seeberger, Peter H.
Published:
Springer Science and Business Media LLC, 2021
Published in:
Scientific Reports, 11 (2021) 1
Language:
English
DOI:
10.1038/s41598-021-93361-y
ISSN:
2045-2322
Origination:
Footnote:
Description:
AbstractEffective 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.