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

• Published in: Planta medica Vol. 74; no. 5; p. 540
• Main Authors: Lv, Liang, Yang, Qing-Yun, Zhao, Ying, Yao, Chun-Suo, Sun, Yang, Yang, Eun-Ju, Song, Kyung-Sik, Mook-Jung, Inhee, Fang, Wei-Shuo
• Format: Journal Article
• Language: English
• Published: Germany 01-04-2008
• Subjects: 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
• ISSN: 0032-0943
• DOI: 10.1055/s-2008-1074496

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.