Identification of SARS-CoV-2 inhibitors using lung and colonic organoids

Nature. 2021 Jan;589(7841):270-275. doi: 10.1038/s41586-020-2901-9. Epub 2020 Oct 28.

Abstract

There is an urgent need to create novel models using human disease-relevant cells to study severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) biology and to facilitate drug screening. Here, as SARS-CoV-2 primarily infects the respiratory tract, we developed a lung organoid model using human pluripotent stem cells (hPSC-LOs). The hPSC-LOs (particularly alveolar type-II-like cells) are permissive to SARS-CoV-2 infection, and showed robust induction of chemokines following SARS-CoV-2 infection, similar to what is seen in patients with COVID-19. Nearly 25% of these patients also have gastrointestinal manifestations, which are associated with worse COVID-19 outcomes1. We therefore also generated complementary hPSC-derived colonic organoids (hPSC-COs) to explore the response of colonic cells to SARS-CoV-2 infection. We found that multiple colonic cell types, especially enterocytes, express ACE2 and are permissive to SARS-CoV-2 infection. Using hPSC-LOs, we performed a high-throughput screen of drugs approved by the FDA (US Food and Drug Administration) and identified entry inhibitors of SARS-CoV-2, including imatinib, mycophenolic acid and quinacrine dihydrochloride. Treatment at physiologically relevant levels of these drugs significantly inhibited SARS-CoV-2 infection of both hPSC-LOs and hPSC-COs. Together, these data demonstrate that hPSC-LOs and hPSC-COs infected by SARS-CoV-2 can serve as disease models to study SARS-CoV-2 infection and provide a valuable resource for drug screening to identify candidate COVID-19 therapeutics.

MeSH terms

  • Animals
  • Antiviral Agents / pharmacology*
  • COVID-19 / prevention & control
  • COVID-19 / virology*
  • COVID-19 Drug Treatment
  • Colon / cytology*
  • Colon / drug effects
  • Colon / virology
  • Drug Approval
  • Drug Evaluation, Preclinical / methods*
  • Female
  • Heterografts / drug effects
  • Humans
  • In Vitro Techniques
  • Lung / cytology*
  • Lung / drug effects
  • Lung / virology
  • Male
  • Mice
  • Organoids / cytology
  • Organoids / drug effects*
  • Organoids / metabolism
  • Organoids / virology*
  • SARS-CoV-2 / drug effects*
  • SARS-CoV-2 / genetics
  • United States
  • United States Food and Drug Administration
  • Viral Tropism
  • Virus Internalization / drug effects

Substances

  • Antiviral Agents