Rat intestinal sucrase inhibited by minor constituents from the leaves and twigs of Archidendron clypearia (Jack.) Nielsen

Bioorg Med Chem Lett. 2016 Sep 1;26(17):4272-6. doi: 10.1016/j.bmcl.2016.07.044. Epub 2016 Jul 21.

Abstract

In the search for plants, containing compounds with α-glucosidase inhibitory activity, we found that a methanolic extract from the leaves and twigs of Archidendron clypearia (Jack.) Nielsen significantly inhibited rat intestinal sucrase in vitro. A phytochemical investigation of the aqueous layer of an A. clypearia extract led to the isolation of 14 compounds (1-14). Their structures were established through extensive 1D and 2D NMR, CD data, and MS analysis. The methanolic extract, as well as the water layer at a concentration of 3.0mg/mL, showed potent sucrase inhibitory activity, with 67.78±2.53% and 95.33±2.15% inhibition, respectively. In addition, compounds 6, 7, and 10 (1.0mM) showed potent sucrase inhibition (88.36±1.15%, 81.57±1.07%, and 66.32±4.73% inhibition, respectively), which was comparable to that of the positive control, acarbose, which exhibited 89.54±0.91% inhibition. Other compounds showed moderate or weak inhibitory activity at the same concentration. The sucrase inhibitory activity of the extracts and purified compounds may provide a novel opportunity to develop a new class of antidiabetic agents.

Keywords: Archidendron clypearia; Arclysides A–B; Fabaceae; Sucrase inhibitory activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Circular Dichroism
  • Fabaceae / chemistry*
  • Intestines / drug effects*
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Plant Extracts / chemistry*
  • Plant Extracts / pharmacology*
  • Plant Leaves / chemistry
  • Plant Stems / chemistry
  • Rats
  • Sucrase / antagonists & inhibitors*

Substances

  • Plant Extracts
  • Sucrase