Potential α-glucosidase inhibitor from Hylotelephium erythrostictum

Bioorg Med Chem Lett. 2020 Dec 15;30(24):127665. doi: 10.1016/j.bmcl.2020.127665. Epub 2020 Nov 2.

Abstract

In light of the adequate sources for Hylotelephium erythrostictum, its active components have aroused research interest. 2-(3',4'-dihydroxyphenyl)-2,3-dihydro-4,6-dihydroxy-2-(methoxy)- 3-benzofuranone(1), apigenin(2), diosmetin(3), kaempferol(4), kaempferide(5), rhamnocitrin(6), quercetin(7), and gallic acid(8) were isolated from H. erythrostictum. Rarely occurring naturally, 1 is 2-methoxybenzofuranone type compound against α-glucosidase and exhibits a potential inhibitory effect on α-glucosidase(IC50 = 1.8 μM), with a Ki value of 709 nM. In silico molecular docking was performed for the investigation of the inhibition mechanism. H. erythrostictum is a potential source of antidiabetic agent. This information is useful in finding more potent antidiabetic candidates from medicinal plants for the clinical development of therapeutics.

Keywords: 2-(Methoxy)-3-benzofuranone; Antidiabetic candidate; Hylotelephium erythrostictum; In silico molecular docking; α-Glucosidase inhibitor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalytic Domain / drug effects
  • Crassulaceae / chemistry*
  • Glycoside Hydrolase Inhibitors / chemistry*
  • Glycoside Hydrolase Inhibitors / pharmacology*
  • Humans
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology
  • Molecular Docking Simulation
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • alpha-Glucosidases / chemistry
  • alpha-Glucosidases / metabolism*

Substances

  • Glycoside Hydrolase Inhibitors
  • Hypoglycemic Agents
  • Plant Extracts
  • alpha-Glucosidases