title: beta-Secretase (BACE-1) inhibitory effect of biflavonoids.
abstract: Here, we describe amentoflavone-type biflavonoids, which were isolated from natural sources and were found to inhibit beta-secretase (BACE-1). The structure-activity relationship was studied, and compounds 1-8, 10, 17, and 18 showed BACE-1 inhibitory activity. Among these compounds, 2,3-dihydroamentoflavone 17 and 2,3-dihydro-6-methylginkgetin 18 exhibited potent inhibitory effects with IC(50) values of 0.75 and 0.35 microM, respectively.
authors.affiliation: School of Pharmacy, Shujitsu University, Naka-ku, Okayama 703-8516, Japan.
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Sasaki
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Miki
authors.forename: Kaoru
authors.initials: K
authors.lastname: Kinoshita
authors.forename: Kiyotaka
authors.initials: K
authors.lastname: Koyama
authors.forename: Lia D
authors.initials: LD
authors.lastname: Juliawaty
authors.forename: Sjamsul A
authors.initials: SA
authors.lastname: Achmad
authors.forename: Euis H
authors.initials: EH
authors.lastname: Hakim
authors.forename: Miyuki
authors.initials: M
authors.lastname: Kaneda
authors.forename: Kunio
authors.initials: K
authors.lastname: Takahashi
mesh_terms: D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D044946:Biflavonoids / Q000737:chemistry* / Q000494:pharmacology; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: C553352:2,3-dihydro-6-methylginkgetin; C553351:2,3-dihydroamentoflavone; D044946:Biflavonoids; D011480:Protease Inhibitors; D053829:Amyloid Precursor Protein Secretases