article · Pathophysiology
Momordica charantia, traditionally used to treat ailments such as diabetes, was examined to understand its mechanisms for maintaining glycaemic control. The evaluation combined computational docking of known phytochemicals with in vivo dietary trials in rats. In computational models, the saponins momordicoside D, cucurbitacin, and charantin were identified as principal compounds binding to Takeda-G-protein-receptor-5, glucagon-like peptide-1 receptor, and dipeptidyl peptidase-4, respectively. In animal trials, incorporating twenty per cent bitter lemon into the diet led to a 295.7 per cent increase in glucagon-like peptide-1 expression, accompanied by an 87.2 per cent decrease in dipeptidyl peptidase-4 expression. The results demonstrate that the plant aids diabetes management by simultaneously activating key metabolic receptors and inhibiting dipeptidyl peptidase-4.
Diabetes management often relies on pathways that stimulate insulin release and control glucose metabolism. By showing how specific components of a traditional medicinal plant stimulate protective hormones while suppressing enzymes that degrade them, this work clarifies the biological basis for bitter melon. It offers defined molecular targets for future therapies aiming to improve blood sugar control.
This work could inform pharmaceutical and nutraceutical developers seeking natural lead compounds for glycaemic control therapies. The identified saponins provide specific candidates for antidiabetic drug discovery programmes. However, because the findings are restricted to computational screening and animal gene expression assays, the work is at an early research stage and remains distant from clinical use or commercial product formulation.
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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.
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DOI: 10.1016/j.pathophys.2018.05.003
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