International Journal of Evergreen Scientific Research
Vol.04, Issue 02 (2021), pp.01-12
Research Paper
ISSN:2664-2409(Print)
77
Copyright ESRC | All Rights Reserved © 2018-2022 Web link: https://ijesrc.com/
In-silico drug design of Zeylanone and its derivatives against 6M0J
for treatment of COVID-19 using molecular docking tools
Md. Shimul Bhuia
1
, Abul Bashar Ripon Khalipha
1,3*
, Naimur Rahman
1
, Md. Golam
Rabbani
1
, Md. Sajjad Hossain Siam
1
, Md. Solayman Hossain
1
, Milon Mondal
1
, Md.
Hanif Munshi
2
, Md. Mozno Mia
2
, Shahadat Hossen
2
1
Department of Pharmacy, Bangabandhu Sheikh Mujibur Rahman Science and
Technology University, Gopalganj-8100, Bangladesh
2
Department of Applied Chemistry and Chemical Engineering, Bangabandhu Sheikh
Mujibur Rahman Science and Technology University, Gopalganj-8100, Bangladesh
3
Evergreen Scientific Research Centre, Gopalganj-8100, Bangladesh
Keyword: Zeylanone, Covid-19, Molecular modeling, SARS-CoV-2, Virtual screening, 6M0J, ACE2
Received: 02-08-2021
Accepted: 14-08-2021
Published: 30-10-2021
*Corresponding Author:
Abul bashar Ripon Khalipha
Email-
khalipha1982@gmail.com
Abstract: The pandemic COVID-19 resulted from the infection of the severe acute
respiratory syndrome corona virus-2 (SARS-CoV-2) has become the most emergent global
health issue. Particular and efficient antiviral therapy against SARS-Cov-2 is still lacking,
so the refinement of effective antiviral drugs against the virus is urgently needed. The
phytochemical Zeylanone (D) extracted from Plumbago zeylanica has strong antiviral
activity with other pharmacological effects. SARS-Cov-2 affects the individual host cell
because of its strong binding affinity with ACE2 of the lung’s epithelial cells by which the
virus enters the host cell. Zeylanone contains a great inhibitory effects against the virus due
to its attaching affinity with the same receptor (ACE2). The aim of this study is to
design better conformer due to the adequate potency and suitable pharmacokinetics of
Zeylanone. We have designed several derivatives and docked them against potential targets
such as ACE2 (PDB ID: 6M0J), the main protease (PDB ID: 6LU7), RNA dependent RNA
polymerase (PDB ID: 7BTF) and PLpro (PDB ID: 7KOL) crystal structures of proteins
collected from the RCSB PDB protein data bank. AutoDockVina was used for docking, and
drug-likeness, toxicity, carcinogenicity as well as pharmacokinetic properties were
evaluated using PreADMET, SwissDrugDesign, and the admetSAR@LMMD online
database. The interaction site between drugs and proteins, pocket size, type and distance of
non-bond interaction were assessed by PyMOL and Discovery Studio visualizer
v4.5.0.15071. Finally, all of the compounds were optimized, and their thermodynamic data
were computed using Gauss View (v5.0). According to our findings, the derivative D3 has
the highest binding value of -10.1 kcal/mol against 6M0J (ACE2), while the parent drug
has a binding value of -8.9 kcal/mol against the same target. The derived drugs formed drug-
protein complexes with various non-bond interactions for example conventional hydrogen
bonds, alkyl bonds, pi-alkyl bonds, and pi-pi T-shaped bonds. All the derivatives ensured
us of their non-toxicity and better pharmacokinetics than the parent drug. According to our
investigation results, D3 (derived drug) can be referred to as a prospective novel inhibitor
against ACE2 for the maintenance and treatment of viral affected patients.