Potential use of bitter melon (Momordica charantia) derived compounds as antidiabetics: In silico and in vivo studies

Olusola Olalekan Elekofehinti; Esther Opeyemi Ariyo; Moses Orimoloye Akinjiyan; Olanrewaju Sam Olayeriju; Akeem Olalekan Lawal; Isaac Gbadura Adanlawo; Joao Batista Teixeira Rocha

doi:10.1016/j.pathophys.2018.05.003

Potential use of bitter melon (Momordica charantia) derived compounds as antidiabetics: In silico and in vivo studies

Pathophysiology. 2018 Dec;25(4):327-333. doi: 10.1016/j.pathophys.2018.05.003.

Authors

Olusola Olalekan Elekofehinti¹, Esther Opeyemi Ariyo², Moses Orimoloye Akinjiyan², Olanrewaju Sam Olayeriju², Akeem Olalekan Lawal², Isaac Gbadura Adanlawo³, Joao Batista Teixeira Rocha⁴

Affiliations

¹ Bioinformatics and Molecular Biology Units, Department of Biochemistry, Federal University of Technology, Akure, Nigeria. Electronic address: ooelekofehinti@futa.edu.ng.
² Bioinformatics and Molecular Biology Units, Department of Biochemistry, Federal University of Technology, Akure, Nigeria.
³ Ekiti State University, Ado Ekiti, Nigeria.
⁴ Bioquimica Toxicologia, Departmento de Quimica, CCNE, Universidade Federal de Santa Maria, RS, 97105-900 Brazil.

PMID: 29764719
DOI: 10.1016/j.pathophys.2018.05.003

Abstract

Momordica charantia (bitter lemon) belongs to the cucurbitaceae family which has been extensively used in traditional medicines for the cure of various ailments such as cancer and diabetes. The underlying mechanism of M. charantia to maintain glycemic control was investigated. GLP-1 and DPP-4 gene modulation by M. charantia (5-20% inclusion in rats diet) was investigated in vivo by RT-PCR and possible compounds responsible for diabetic action predicted through in silico approach. Phytochemicalss previously characterized from M. charantia were docked into glucacon like peptide-1 receptor (GLP-1r), dipeptidyl peptidase (DPP4) and Takeda-G-protein-receptor-5 (TGR5) predicted using Autodock Vina. The results of the in silico suggests momordicosides D (ligand for TGR5), cucurbitacin (ligand for GLP-1r) and charantin (ligand for DPP-4) as the major antidiabetic compounds in bitter lemon leaf. M. charantia increased the expression of GLP-1 by about 295.7% with concomitant decreased in expression of DPP-4 by 87.2% with 20% inclusion in rat's diet. This study suggests that the mechanism underlying the action of these compounds is through activation of TGR5 and GLP-1 receptor with concurrent inhibition of DPP4. This study confirmed the use of this plant in diabetes management and the possible bioactive compounds responsible for its antidiabetic property are charantin, cucurbitacin and momordicoside D and all belong to the class of saponins.

Keywords: Bitter lemon; DPP4; Gene expression; Glp-1; Molecular docking; TGR5.