Anti-SARS-CoV-2 Potential of Artemisinins In Vitro

ACS Infect Dis. 2020 Sep 11;6(9):2524-2531. doi: 10.1021/acsinfecdis.0c00522. Epub 2020 Aug 18.


The discovery of novel drug candidates with anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) potential is critical for the control of the global COVID-19 pandemic. Artemisinin, an old antimalarial drug derived from Chinese herbs, has saved millions of lives. Artemisinins are a cluster of artemisinin-related drugs developed for the treatment of malaria and have been reported to have multiple pharmacological activities, including anticancer, antiviral, and immune modulation. Considering the reported broad-spectrum antiviral potential of artemisinins, researchers are interested in whether they could be used to combat COVID-19. We systematically evaluated the anti-SARS-CoV-2 activities of nine artemisinin-related compounds in vitro and carried out a time-of-drug-addition assay to explore their antiviral mode of action. Finally, a pharmacokinetic prediction model was established to predict the therapeutic potential of selected compounds against COVID-19. Arteannuin B showed the highest anti-SARS-CoV-2 potential with an EC50 of 10.28 ± 1.12 μM. Artesunate and dihydroartemisinin showed similar EC50 values of 12.98 ± 5.30 μM and 13.31 ± 1.24 μM, respectively, which could be clinically achieved in plasma after intravenous administration. Interestingly, although an EC50 of 23.17 ± 3.22 μM was not prominent among the tested compounds, lumefantrine showed therapeutic promise due to high plasma and lung drug concentrations after multiple dosing. Further mode of action analysis revealed that arteannuin B and lumefantrine acted at the post-entry step of SARS-CoV-2 infection. This research highlights the anti-SARS-CoV-2 potential of artemisinins and provides leading candidates for anti-SARS-CoV-2 drug research and development.

Keywords: COVID-19; SARS-CoV-2; antiviral drug; artemisinin; drug repurposing.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / pharmacology
  • Antiviral Agents / pharmacology*
  • Artemisinins / pharmacology*
  • Betacoronavirus / drug effects*
  • COVID-19
  • Chlorocebus aethiops
  • Coronavirus Infections / drug therapy*
  • Coronavirus Infections / virology*
  • Drug Discovery
  • Drug Repositioning
  • Drugs, Chinese Herbal / pharmacology
  • Pandemics
  • Pneumonia, Viral / drug therapy*
  • Pneumonia, Viral / virology*
  • SARS-CoV-2
  • Vero Cells


  • Antimalarials
  • Antiviral Agents
  • Artemisinins
  • Drugs, Chinese Herbal