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, (+)-epsilon-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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Amyloid Precursor Protein Secretases / antagonists & inhibitors
-
Antioxidants / isolation & purification
-
Antioxidants / pharmacology*
-
Aspartic Acid Endopeptidases / antagonists & inhibitors
-
Baculoviridae
-
Enzyme Inhibitors / isolation & purification
-
Enzyme Inhibitors / pharmacology*
-
Molecular Structure
-
Plant Bark
-
Plant Extracts / chemistry
-
Plant Extracts / isolation & purification
-
Plant Extracts / pharmacology*
-
Plant Stems
-
Resveratrol
-
Stilbenes / isolation & purification
-
Stilbenes / pharmacology*
-
Vitis / chemistry*
Substances
-
Antioxidants
-
Enzyme Inhibitors
-
Plant Extracts
-
Stilbenes
-
Amyloid Precursor Protein Secretases
-
Aspartic Acid Endopeptidases
-
BACE1 protein, human
-
Resveratrol