- beta-Secretase (BACE-1) inhibitory effect of biflavonoids.
beta-Secretase (BACE-1) inhibitory effect of biflavonoids.
Bioorganic & medicinal chemistry letters (2010-07-06)
Hiroaki Sasaki, Kazuhiko Miki, Kaoru Kinoshita, Kiyotaka Koyama, Lia D Juliawaty, Sjamsul A Achmad, Euis H Hakim, Miyuki Kaneda, Kunio Takahashi
PMID20598535
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.
MATERIALS