A new specific BACE-1 inhibitor from the stembark extract of Vitis vinifera.
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.
Choi
Yeon Hee
YH
Korea Research Institute of Chemical Technology, Daejeon, Korea.
Yoo
Mi Young
MY
Choi
Chun Whan
CW
Cha
Mi-Ran
MR
Yon
Gyu Hwan
GH
Kwon
Dae Young
DY
Kim
Young Sup
YS
Park
Woo-Kyu
WK
Ryu
Shi Yong
SY
D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors; D000975:Antioxidants / Q000302:isolation & purification / Q000494:pharmacology*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors; D016367:Baculoviridae; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D015394:Molecular Structure; D024301:Plant Bark; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018547:Plant Stems; D000077185:Resveratrol; D013267:Stilbenes / Q000302:isolation & purification / Q000494:pharmacology*; D027843:Vitis / Q000737:chemistry*
D000975:Antioxidants; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D013267:Stilbenes; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human; D000077185:Resveratrol