In vitro BACE-1 inhibitory activity of resveratrol oligomers from the seed extract of Paeonia lactiflora.
A new resveratrol oligomer (1) together with eight related components (2- 9) were isolated from the seed extract of Paeonia lactiflora (Paeoniaceae) as active principles responsible for the inhibition of beta-site APP-cleaving enzyme 1 (BACE-1) in vitro. The chemical structure of 1 was established as (-)-7a,8a- CIS- ε-viniferin with the aid of spectroscopic analyses including NOESY experiments. All isolated resveratrol oligomers (1- 9) demonstrated significant inhibition on baculovirus-expressed BACE-1 in a dose-dependent manner, which was assessed by the FRET assay using Rh-EVNLDAEFK as a substrate in vitro.
Choi
Chun Whan
CW
Korea Research Institute of Chemical Technology, Daejeon, Korea.
Choi
Yeon Hee
YH
Cha
Mi-Ran
MR
Kim
Young Sup
YS
Yon
Gyu Hwan
GH
Hong
Kyung Sik
KS
Park
Woo-Kyu
WK
Kim
Young Ho
YH
Ryu
Shi Yong
SY
D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D016367:Baculoviridae; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015394:Molecular Structure; D029596:Paeonia / Q000737:chemistry*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D000077185:Resveratrol; D012639:Seeds; D013267:Stilbenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
C562102:7a,8a-cis-epsilon-viniferin; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D013267:Stilbenes; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human; D000077185:Resveratrol