411
The Journal of Phytopharmacology 2023; 12(6):411-420
Online at: www.phytopharmajournal.com
Research Article
ISSN 2320-480X
JPHYTO 2023; 12(6): 411-420
November- December
Received: 02-10-2023
Accepted: 24-12-2023
©2023, All rights reserved
doi: 10.31254/phyto.2023.12607
Ololade Zacchaeus S
Department of Chemistry, Medicinal
and Organic Chemistry Unit, University
of Medical Sciences, Ondo, Nigeria
Lajide Labunmi
Department of Chemistry, Medicinal
and Organic Chemistry Unit, University
of Medical Sciences, Ondo, Nigeria
Onifade Olayinka F
Department of Chemical Sciences,
Biochemistry Unit, Bells University of
Technology, Ota, Nigeria
Eze John C
Department of Chemistry, Medicinal
and Organic Chemistry Unit, University
of Medical Sciences, Ondo, Nigeria
Tommy Bessie E
Department of Chemistry, Medicinal
and Organic Chemistry Unit, University
of Medical Sciences, Ondo, Nigeria
Orodepo Gabriel O
Department of Chemistry, Medicinal
and Organic Chemistry Unit, University
of Medical Sciences, Ondo, Nigeria
Idowu Olaniyi O
Department of Chemistry, Medicinal
and Organic Chemistry Unit, University
of Medical Sciences, Ondo, Nigeria
Oyebanji Olawumi T
Department of Chemistry, Medicinal
and Organic Chemistry Unit, University
of Medical Sciences, Ondo, Nigeria
Olaniran Anikeola C
Department of Chemistry, Medicinal
and Organic Chemistry Unit, University
of Medical Sciences, Ondo, Nigeria
Correspondence:
Dr. Ololade Zacchaeus S
Department of Chemistry, Medicinal
and Organic Chemistry Unit, University
of Medical Sciences, Ondo, Nigeria
Email: sololade@unimed.edu.ng
Exploration of Secondary Metabolites in Flower-Petal
Annona muricata as Agonists for Peroxisome Proliferator-
Activated Receptor-Alpha (PPARα) for Liver Function
Ololade Zacchaeus S, Lajide Labunmi, Onifade Olayinka F, Eze John C, Tommy Bessie E, Orodepo
Gabriel O, Idowu Olaniyi O, Oyebanji Olawumi T, Olaniran Anikeola C
ABSTRACT
The expression of PPARα in the liver is significantly increased in both non-alcoholic fatty liver disease
(NAFLD) patients and experimental models. Animal studies have shown promising outcomes in
improving histological conditions, such as fibrosis, through the use of PPARα agonists. This particular
petal to act as agonists for PPARα. Molecular docking and Prime MM-GBSA (Molecular Mechanics-
Generalized Born Surface Area) were employed to analyze the ligand binding affinity, atomistic
interactions, and protein stability. Additionally, we conducted evaluations of the identified PPARα
agonist candidates to assess their toxicity and pharmacological profiles were conducted. The hit
compounds exhibit favourable binding affinity and thermodynamics stability, and interact effectively
with key residues in the binding site. Furthermore, the safety assessment indicates minimal to non-acute
toxicity and favourable drug-like properties for these compounds. Secondary metabolites in the extract
are potential drug candidate. They demonstrate drug-like properties as they adhere to the Lipinski rule.
Keywords: Annona muricata, Flower-petal, Phytochemicals, PPARα, ADMET, Liver function,
Lipinski rule.
INTRODUCTION
Natural products from medicinal plants are good sources for deriving phytochemical for drug
development
[1-3]
. Phytochemicals have been produced in the various environment, which represents an
alternative resource for new drugs used to treat diseases
[4-6]
. Natural products remain as a leading source
for the development of pharmaceuticals
[6-8]
. Annona muricata (sour sop) is a medicinal plant known as a
natural multipurpose phytotherapy agent
[9,10]
. A. muricata is locally used to treat mesenteric
lymphadentis, gastrointerstinal disorders, fever, rheumatoid, gouty, joints pain, skin ailments,
tuberculosis, nausea, neurological disorders, bacterial and fungal infections, respiratory illnesses,
diabetes, parasites and so on
[10,11]
. Peroxisome proliferator-activated receptor (PPAR) α, β/δ, and γ
modulate lipid homeostasis. PPARα Peroxisome proliferator-activated receptor-α (PPARα) is a nuclear
hormone receptor which regulates the oxidation and transport of fatty acids. Upon activation it binds as a
heterodimer with retinoid X receptor (RXR) to peroxisome response elements in genes involved in fatty
acid oxidation. PPARα/γ activation might decrease the hepatic lipid accumulation, oxidative stress and
inflammatory cytokine production
[12-14]
. Peroxisome proliferator-activated receptor (PPAR) α, β/δ, and γ
modulate lipid homeostasis. In liver, PPARα regulates lipid metabolism in the liver, the organ that
largely controls whole-body nutrient/energy homeostasis, and its abnormalities may lead to hepatic
steatosis, steatohepatitis, steatofibrosis, and liver cancer
[15-17]
. To the best of our knowledge, there is
paucity information on the use of phytochemicals as agonists for peroxisome proliferator-activated
receptor-alpha (PPARα) so far. This study assessed their agonistic properties by comparing their binding
affinity, binding interactions, and binding energy to a known agonist, fenofibrate and saroglitazar.
Therefore, the research showcased the exploration of secondary metabolites in flower-petal extract of A.
muricata as agonists for peroxisome proliferator-activated receptor-alpha (PPARα) for liver function.
MATERIALS AND METHODS
Protein retrieval and preparation
The 3D crystal structure of Peroxisome proliferator-activated receptor alpha (PPARα) was obtained from
the Protein Data Bank (PDB ID = 2ZNN) via their website (http://www.rcsb.org/pdb). The protein was
prepared and visualized using the Protein Preparation Wizard panel in the Schrödinger Maestro suite
11.5
[18]
. The preparation involved filling in missing loops and side chains using Prime, establishing