Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In Vitro

Molecules. 2022 Jan 21;27(3):712. doi: 10.3390/molecules27030712.

Abstract

COVID-19 has spread around the world and caused serious public health and social problems. Although several vaccines have been authorized for emergency use, new effective antiviral drugs are still needed. Some repurposed drugs including Chloroquine, Hydroxychloroquine and Remdesivir were immediately used to treat COVID-19 after the pandemic. However, the therapeutic effects of these drugs have not been fully demonstrated in clinical studies. In this paper, we found an antimalarial drug, Naphthoquine, showed good broad-spectrum anti-coronavirus activity. Naphthoquineinhibited HCoV-229E, HCoV-OC43 and SARS-CoV-2 replication in vitro, with IC50 = 2.05 ± 1.44 μM, 5.83 ± 0.74 μM, and 2.01 ± 0.38 µM, respectively. Time-of-addition assay was also performed to explore at which stage Naphthoquine functions during SARS-CoV-2 replication. The results suggested that Naphthoquine may influence virus entry and post-entry replication. Considering the safety of Naphthoquine was even better than that of Chloroquine, we think Naphthoquine has the potential to be used as a broad-spectrum drug for coronavirus infection.

Keywords: Naphthoquine; SARS-CoV-2; coronavirus; malaria; repurposing.

MeSH terms

  • 1-Naphthylamine / analogs & derivatives*
  • 1-Naphthylamine / pharmacology
  • Aminoquinolines / pharmacology*
  • Animals
  • Antiviral Agents / pharmacology*
  • Cell Line
  • Chlorocebus aethiops
  • Coronavirus / drug effects*
  • Coronavirus 229E, Human / drug effects
  • Coronavirus NL63, Human / drug effects
  • Coronavirus OC43, Human / drug effects
  • Humans
  • In Vitro Techniques
  • SARS-CoV-2 / drug effects*
  • Vero Cells
  • Virus Replication / drug effects

Substances

  • Aminoquinolines
  • Antiviral Agents
  • naphthoquine
  • 1-Naphthylamine