A New Specific BACE-1 Inhibitor from the Stembark Extract of Vitis vinifera

Abstract

A new resveratrol dimer, (+)-vitisinol E (1) which demonstrated inhibitory activity on BACE-1 (beta-site APP-cleaving enzyme 1) in vitro, was isolated from the stembark extract of Vitis vinifera (Vitaceae) together with four known resveratrol oligomers, (+)-ε-viniferin (2), (+)-ampelopsin A (3), (+)-vitisin A (4) and (−)-vitisin B (5). The chemical structure of 1 was established by MR spectroscopic analyses, including HMBC. All isolated resveratrol derivatives (1–5) demonstrated significant inhibition on baculovirus-expressed BACE-1 in a dose-dependent manner, which was assessed with the FRET assay using Rh-EVNLDAEFK as a substrate in vitro.

resveratrol dimer - Vitis vinifera - Vitaceae - BACE‐1 inhibition

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