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

作者:Choi Yeon Hee; Yoo Mi Young; Choi Chun Whan; Cha Mi Ran; Yon Gyu Hwan; Kwon Dae Young; Kim Young Sup; Park Woo Kyu; Ryu Shi Yong*
来源:Planta Medica, 2009, 75(5): 537-540.
DOI:10.1055/s-0029-1185311

摘要

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, ( )-epsilon-viniferin (2), ( )-ampelopsin A (3), ( )-vitisin A (4) and (-)-vitisin B (5). The chemical structure of I 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.

  • 出版日期2009-4