BACE1 (β-Secretase) Inhibitory Chromone Glycosides from Aloe vera and Aloe nobilis

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 (β-secretase) with IC₅₀ values of 39.0 and 20.5 × 10^-6 M, as well as inhibition of Aβ_{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.

Aloe vera - Aloe nobilis - Liliaceae - chromone glycosides - BACE1 (β-secretase) inhibitor - Alzheimer’s disease (AD)

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1 Equal contributions to this work.