Phytoconstituents as potential therapeutic agents against COVID-19: a computational study on inhibition of SARS-CoV-2 main protease

J Biomol Struct Dyn. 2024;42(19):10539-10550. doi: 10.1080/07391102.2023.2257328. Epub 2023 Sep 15.

Abstract

The Coronavirus disease 2019 (COVID-19) pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS‑CoV‑2) has become a global health crisis, and the urgent need for effective treatments is evident. One potential target for COVID-19 therapeutics is the main protease (Mpro) of SARS‑CoV‑2, an essential enzyme for viral replication. Natural compounds have been explored as a source of potential inhibitors for Mpro due to their safety and availability. In this study, we employed a computational approach to screen a library of phytoconstituents and identified potential Mpro inhibitors based on their binding affinities and molecular interactions. The top-ranking compounds were further validated through molecular dynamics simulations (MDS) and free energy calculations. As a result of the above procedures, we identified two phytoconstituents, Khelmarin B and Neogitogenin, with appreciable binding affinity and specificity towards the Mpro binding pocket. Our results suggest that Khelmarin B and Neogitogenin could potentially serve as Mpro inhibitors and have the potential to be developed as COVID-19 therapeutics. Further experimental studies are required to confirm the efficacy and safety of these compounds.Communicated by Ramaswamy H. Sarma.

Keywords: COVID-19; Khelmarin B; Natural compounds; Neogitogenin; Phytonutrients; SARS-CoV-2 main protease; drug discovery.

MeSH terms

  • Antiviral Agents* / chemistry
  • Antiviral Agents* / pharmacology
  • Binding Sites
  • COVID-19 / virology
  • COVID-19 Drug Treatment*
  • Coronavirus 3C Proteases* / antagonists & inhibitors
  • Coronavirus 3C Proteases* / chemistry
  • Coronavirus 3C Proteases* / metabolism
  • Humans
  • Molecular Docking Simulation*
  • Molecular Dynamics Simulation*
  • Phytochemicals / chemistry
  • Phytochemicals / pharmacology
  • Protease Inhibitors* / chemistry
  • Protease Inhibitors* / pharmacology
  • Protein Binding
  • SARS-CoV-2* / drug effects
  • SARS-CoV-2* / enzymology
  • Thermodynamics

Substances

  • Coronavirus 3C Proteases
  • Antiviral Agents
  • Protease Inhibitors
  • Phytochemicals