Insight into Gentisic Acid Antidiabetic Potential Using In Vitro and In Silico Approaches

Molecules. 2021 Mar 30;26(7):1932. doi: 10.3390/molecules26071932.

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.

Keywords: AldR; DPP4; FFAR1; GP; PPAR-γ; PTP1B; gentisic acid; in silico; in vitro; molecular docking; α-amylase; α-glucosidase.

MeSH terms

  • Fruit / chemistry*
  • Gentisates / metabolism*
  • Glycoside Hydrolase Inhibitors / metabolism*
  • Humans
  • Hypoglycemic Agents / metabolism*
  • Molecular Docking Simulation
  • Protein Binding
  • alpha-Amylases* / antagonists & inhibitors
  • alpha-Amylases* / metabolism
  • alpha-Glucosidases / metabolism*

Substances

  • Gentisates
  • Glycoside Hydrolase Inhibitors
  • Hypoglycemic Agents
  • alpha-Amylases
  • alpha-Glucosidases
  • 2,5-dihydroxybenzoic acid