Publikationsdatenbank

In vitro efficacy of artemisinin-based treatments against SARS-CoV-2 (2021)

Art

Zeitschriftenartikel / wissenschaftlicher Beitrag

Autoren

Zhou, Yuyong

Gilmore, Kerry

Ramirez, Santseharay

Settels, Eva

Gammeltoft, Karen A.

Pham, Long V.

Fahnøe, Ulrik

Feng, Shan

Offersgaard, Anna

Trimpert, Jakob (WE 5)

Bukh, Jens

Osterrieder, Klaus (WE 5)

Gottwein, Judith M.

Seeberger, Peter H.

Quelle

Scientific reports

Bandzählung: 11

Heftzählung: 1

Seiten: Article number: 14571

ISSN: 2045-2322

Sprache

Englisch

Verweise

URL (Volltext): https://www.nature.com/articles/s41598-021-93361-y

DOI: 10.1038/s41598-021-93361-y

Pubmed: 34272426

Kontakt

Institut für Virologie

Robert-von-Ostertag-Str. 7-13
14163 Berlin
+49 30 838 51833
virologie@vetmed.fu-berlin.de

Abstract / Zusammenfassung

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.