BACE1 (beta-secretase) inhibitory chromone glycosides from Aloe vera and Aloe nobilis

Planta Med. 2008 Apr;74(5):540-5. doi: 10.1055/s-2008-1074496.

Abstract

Four new chromone glycosides allo-aloeresin D (2) , C-2'-decoumaroyl-aloeresin G (8), 2'-O-coumaroyl-(S)-aloesinol (9), 2'-O-[ P-methoxy-(E)-cinnamoyl]-(S)-aloesinol (10) and nine known chromone glycosides ( 1, 3 - 7, 11 - 13) were isolated from two Aloe spp. plants, A. vera and A. nobilis. Among them, 1 and 8 showed significant inhibitory activity against BACE1 (beta-secretase) with IC (50) values of 39.0 and 20.5 x 10 (-6) M, as well as inhibition of Abeta (1-42) production by 7.4 and 12.3 %, respectively, in B103 neuroblastoma cells at 30 ppm. The preliminary structure-activity relationships of ALOE chromone glucosides were also discussed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aloe / chemistry*
  • Amyloid Precursor Protein Secretases / antagonists & inhibitors*
  • Aspartic Acid Endopeptidases / antagonists & inhibitors*
  • Chromones / chemistry
  • Chromones / isolation & purification*
  • Glycosides / chemistry
  • Glycosides / isolation & purification*
  • Molecular Structure

Substances

  • Chromones
  • Glycosides
  • Amyloid Precursor Protein Secretases
  • Aspartic Acid Endopeptidases
  • BACE1 protein, human