Evaluation of Major Constituents of Medicinally Important Plants for Anti-Inflammatory, Antidiabetic and AGEs Inhibiting Properties: In Vitro and Simulatory Evidence

Molecules. 2022 Oct 9;27(19):6715. doi: 10.3390/molecules27196715.

Abstract

Diabetes mellitus (DM) is a global health concern that is associated with several micro- and macrovascular complications. We evaluated several important medicinal plant constituents, including polyphenols and flavonoids, for α-glucosidase inhibition, AGEs' inhibitory activities using oxidative and no-oxidative assays, the inhibition of protein cross link formation, 15-lipoxydenase inhibition and molecular docking. The molecular docking studies showed high binding energies of flavonoids for transcriptional regulars 1IK3, 3TOP and 4F5S. In the α-glucosidase inhibition assay, a significant inhibition was noted for quercitrin (IC50 7.6 µg/mL) and gallic acid (IC50 8.2 µg/mL). In the AGEs inhibition assays, quercetin showed significant results in both non-oxidative and (IC50 0.04 mg/mL) and oxidative assays (IC50 0.051 mg/mL). Furthermore, quercitrin showed inhibitory activity in the non-oxidative (IC50 0.05 mg/mL) and oxidative assays (IC50 0.34 mg/mL). A significant inhibition of protein cross link formation was observed by SDS-PAGE analysis. Quercitrin (65%) and quercetin (62%) showed significant inhibition of 15-lipoxygenase. It was thus concluded that flavonoids and other polyphenols present in plant extracts can be effective in management of diabetes and allied co-morbidities.

Keywords: Punica granatum peel; advanced glycation end products (AGEs); diabetes mellitus; methylglyoxal; protein cross link formation.

MeSH terms

  • Anti-Inflammatory Agents / pharmacology
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Arachidonate 15-Lipoxygenase
  • Diabetes Mellitus*
  • Flavonoids / pharmacology
  • Gallic Acid / pharmacology
  • Glycoside Hydrolase Inhibitors / chemistry
  • Glycoside Hydrolase Inhibitors / pharmacology
  • Humans
  • Hypoglycemic Agents* / chemistry
  • Hypoglycemic Agents* / pharmacology
  • Molecular Docking Simulation
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • Polyphenols / pharmacology
  • Quercetin / pharmacology
  • alpha-Glucosidases / metabolism

Substances

  • Anti-Inflammatory Agents
  • Antioxidants
  • Flavonoids
  • Glycoside Hydrolase Inhibitors
  • Hypoglycemic Agents
  • Plant Extracts
  • Polyphenols
  • Gallic Acid
  • Quercetin
  • Arachidonate 15-Lipoxygenase
  • alpha-Glucosidases

Grants and funding

This research was funded by GA Society for Medicinal Plant and Natural Products Research and the Foundation “Plants for Health”.