Natural Products-Based Drug Design against SARS-CoV-2 Mpro 3CLpro

Int J Mol Sci. 2021 Oct 29;22(21):11739. doi: 10.3390/ijms222111739.

Abstract

Coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has received global attention due to the serious threat it poses to public health. Since the outbreak in December 2019, millions of people have been affected and its rapid global spread has led to an upsurge in the search for treatment. To discover hit compounds that can be used alone or in combination with repositioned drugs, we first analyzed the pharmacokinetic and toxicological properties of natural products from Brazil's semiarid region. After, we analyzed the site prediction and druggability of the SARS-CoV-2 main protease (Mpro), followed by docking and molecular dynamics simulation. The best SARS-CoV-2 Mpro complexes revealed that other sites were accessed, confirming that our approach could be employed as a suitable starting protocol for ligand prioritization, reinforcing the importance of catalytic cysteine-histidine residues and providing new structural data that could increase the antiviral development mainly against SARS-CoV-2. Here, we selected 10 molecules that could be in vitro assayed in response to COVID-19. Two compounds (b01 and b02) suggest a better potential for interaction with SARS-CoV-2 Mpro and could be further studied.

Keywords: 3CLpro; ADMET properties; COVID-19; docking; druggability; molecular dynamics; natural products.

MeSH terms

  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Binding Sites
  • Biological Products / pharmacology*
  • COVID-19 Drug Treatment*
  • Coronavirus 3C Proteases / chemistry*
  • Coronavirus 3C Proteases / drug effects*
  • Drug Design*
  • Drug Discovery / methods
  • Drug Repositioning
  • Humans
  • Ligands
  • Molecular Docking Simulation
  • Molecular Dynamics Simulation
  • Protein Conformation
  • SARS-CoV-2 / chemistry*
  • SARS-CoV-2 / drug effects*
  • Viral Nonstructural Proteins / chemistry
  • Viral Nonstructural Proteins / drug effects

Substances

  • Antiviral Agents
  • Biological Products
  • Ligands
  • Viral Nonstructural Proteins
  • Coronavirus 3C Proteases