Abstract
Numerous scientific studies have confirmed the beneficial therapeutic effects of phenolic acids. Among them gentisic acid (GA), a phenolic acid extensively found in many fruit and vegetables has been associated with an enormous confirmed health benefit. The present study aims to evaluate the antidiabetic potential of gentisic acid and highlight its mechanisms of action following in silico and in vitro approaches. The in silico study was intended to predict the interaction of GA with eight different receptors highly involved in the management and complications of diabetes (dipeptidyl-peptidase 4 (DPP4), protein tyrosine phosphatase 1B (PTP1B), free fatty acid receptor 1 (FFAR1), aldose reductase (AldR), glycogen phosphorylase (GP), α-amylase, peroxisome proliferator-activated receptor gamma (PPAR-γ) and α-glucosidase), while the in vitro study studied the potential inhibitory effect of GA against α-amylase and α-glucosidase. The results indicate that GA interacted moderately with most of the receptors and had a moderate inhibitory activity during the in vitro tests. The study therefore encourages further in vivo studies to confirm the given results.
Highlights
This study was undertaken (i) to reveal the potential action of gentisic acid as an antidiabetic molecule using in vitro methods (ii) assessing its ability to inhibit the α-amylase and α-glucosidase activities and in silico, (iii) studying its mode of action using molecular docking against eight receptors that have a direct impact on the overall status of diabetes (dipeptidyl-peptidase 4 (DPP4), protein tyrosine phosphatase 1B (PTP1B), free fatty acid receptor 1 (FFAR1), aldose reductase (AldR), glycogen phosphorylase (GP), α-amylase (AAM), peroxisome proliferator-activated receptor gamma (PPAR-γ), and α-glucosidase)
The receptors selected for this research were strongly involved in the complications and treatments of diabetes
Located on multiple cell surfaces, with vari adenosine deaminase complexing protein 2 (ADCP 2) and T-c dipeptidyl-peptidase 4 (DPP4) is classified as a serine exopep ily) whose main activity is to cleave X-proline dipeptides fr peptides such as growth factors, neuropeptides and incretin important regulators of postprandial insulin secretion) [19]
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Medicinal plants and natural products have gained more popularity in the field of drug discovery, with many active compounds studied and pharmacologically approved within the past decade [1]. Plant-derived bioactive molecules were subjected to profound studies to discover the relationship between the chemical composition and pharmacological activities, leading to (i) substantial progress in the design and (ii) synthesis of new compounds and amelioration of their pharmacokinetics and pharmacodynamics proprieties [5]. This study was undertaken (i) to reveal the potential action of gentisic acid as an antidiabetic molecule using in vitro methods (ii) assessing its ability to inhibit the α-amylase and α-glucosidase activities and in silico, (iii) studying its mode of action using molecular docking against eight receptors that have a direct impact on the overall status of diabetes (dipeptidyl-peptidase 4 (DPP4), protein tyrosine phosphatase 1B (PTP1B), free fatty acid receptor 1 (FFAR1), aldose reductase (AldR), glycogen phosphorylase (GP), α-amylase (AAM), peroxisome proliferator-activated receptor gamma (PPAR-γ), and α-glucosidase)
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