beta-Secretase (BACE-1) inhibitory effect of biflavonoids.
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.
Sasaki
Hiroaki
H
School of Pharmacy, Shujitsu University, Naka-ku, Okayama 703-8516, Japan.
Miki
Kazuhiko
K
Kinoshita
Kaoru
K
Koyama
Kiyotaka
K
Juliawaty
Lia D
LD
Achmad
Sjamsul A
SA
Hakim
Euis H
EH
Kaneda
Miyuki
M
Takahashi
Kunio
K
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
C553352:2,3-dihydro-6-methylginkgetin; C553351:2,3-dihydroamentoflavone; D044946:Biflavonoids; D011480:Protease Inhibitors; D053829:Amyloid Precursor Protein Secretases