title: 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, (+)-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.
authors.affiliation: Korea Research Institute of Chemical Technology, Daejeon, Korea.
authors.forename: Yeon Hee
authors.initials: YH
authors.lastname: Choi
authors.forename: Mi Young
authors.initials: MY
authors.lastname: Yoo
authors.forename: Chun Whan
authors.initials: CW
authors.lastname: Choi
authors.forename: Mi-Ran
authors.initials: MR
authors.lastname: Cha
authors.forename: Gyu Hwan
authors.initials: GH
authors.lastname: Yon
authors.forename: Dae Young
authors.initials: DY
authors.lastname: Kwon
authors.forename: Young Sup
authors.initials: YS
authors.lastname: Kim
authors.forename: Woo-Kyu
authors.initials: WK
authors.lastname: Park
authors.forename: Shi Yong
authors.initials: SY
authors.lastname: Ryu
mesh_terms: 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*
chemical_list: 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