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Tomatidine and Patchouli Alcohol as Inhibitors of SARS-CoV-2 Enzymes (3CLpro, PLpro and NSP15) by Molecular Docking and Molecular Dynamics Simulations.
- Source :
-
International journal of molecular sciences [Int J Mol Sci] 2021 Oct 02; Vol. 22 (19). Date of Electronic Publication: 2021 Oct 02. - Publication Year :
- 2021
-
Abstract
- Considering the current dramatic and fatal situation due to the high spreading of SARS-CoV-2 infection, there is an urgent unmet medical need to identify novel and effective approaches for prevention and treatment of Coronavirus disease (COVID 19) by re-evaluating and repurposing of known drugs. For this, tomatidine and patchouli alcohol have been selected as potential drugs for combating the virus. The hit compounds were subsequently docked into the active site and molecular docking analyses revealed that both drugs can bind the active site of SARS-CoV-2 3CLpro, PLpro, NSP15, COX-2 and PLA2 targets with a number of important binding interactions. To further validate the interactions of promising compound tomatidine, Molecular dynamics study of 100 ns was carried out towards 3CLpro, NSP15 and COX-2. This indicated that the protein-ligand complex was stable throughout the simulation period, and minimal backbone fluctuations have ensued in the system. Post dynamic MM-GBSA analysis of molecular dynamics data showed promising mean binding free energy 47.4633 ± 9.28, 51.8064 ± 8.91 and 54.8918 ± 7.55 kcal/mol, respectively. Likewise, in silico ADMET studies of the selected ligands showed excellent pharmacokinetic properties with good absorption, bioavailability and devoid of toxicity. Therefore, patchouli alcohol and especially, tomatidine may provide prospect treatment options against SARS-CoV-2 infection by potentially inhibiting virus duplication though more research is guaranteed and secured.
- Subjects :
- Antiviral Agents pharmacology
COVID-19 virology
Coronavirus 3C Proteases metabolism
Coronavirus Papain-Like Proteases metabolism
Endoribonucleases metabolism
Enzyme Inhibitors pharmacology
Humans
Molecular Docking Simulation
Molecular Dynamics Simulation
SARS-CoV-2 drug effects
Tomatine pharmacology
Viral Nonstructural Proteins metabolism
COVID-19 Drug Treatment
Coronavirus 3C Proteases antagonists & inhibitors
Coronavirus Papain-Like Proteases antagonists & inhibitors
Endoribonucleases antagonists & inhibitors
SARS-CoV-2 enzymology
Sesquiterpenes pharmacology
Tomatine analogs & derivatives
Viral Nonstructural Proteins antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1422-0067
- Volume :
- 22
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- International journal of molecular sciences
- Publication Type :
- Academic Journal
- Accession number :
- 34639036
- Full Text :
- https://doi.org/10.3390/ijms221910693