title: Beta-secretase (BACE1)-inhibiting stilbenoids from Smilax Rhizoma.
abstract: In the course of searching for BACE1 (beta-secretase) inhibitors from natural products, the ethyl acetate soluble fraction of Smilax Rhizoma (the dried rhizomes of Smilax china L.) showed potent inhibitory activity. The active compounds were identified as a trans/cis-resveratrol mixture, oxyresveratrol, veraphenol, and cis-scirpusin A. They were shown to non-competitively inhibit BACE1 with the Ki values of 5.4 x 10(-6), 5.4 x 10(-6), 3.4 x 10(-6), and 5.4 x 10(-6)M and IC(50) values of 1.5 x 10(-5), 7.6 x 10(-6), 4.2 x 10(-6), and 1.0 x 10(-5)M, respectively. The active compounds were less inhibitory to alpha-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, suggesting that they were relatively specific inhibitors of BACE1.
authors.affiliation: Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University, 1370 Sankyuk-Dong, Daegu 702-701, Republic of Korea.
authors.forename: S-Y
authors.initials: SY
authors.lastname: Jeon
authors.forename: S-H
authors.initials: SH
authors.lastname: Kwon
authors.forename: Y-H
authors.initials: YH
authors.lastname: Seong
authors.forename: K
authors.initials: K
authors.lastname: Bae
authors.forename: J-M
authors.initials: JM
authors.lastname: Hur
authors.forename: Y-Y
authors.initials: YY
authors.lastname: Lee
authors.forename: D-Y
authors.initials: DY
authors.lastname: Suh
authors.forename: K-S
authors.initials: KS
authors.lastname: Song
mesh_terms: D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D027343:Rhizome / Q000737:chemistry*; D032281:Smilax / Q000737:chemistry*; D013267:Stilbenes / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D013267:Stilbenes; D053829:Amyloid Precursor Protein Secretases