β-Secretase (BACE-1) inhibitory effect of biflavonoids

被引：61

作者：

Sasaki, Hiroaki ^{[2
]}

Miki, Kazuhiko ^{[1
]}

Kinoshita, Kaoru ^{[1
]}

Koyama, Kiyotaka ^{[1
]}

Juliawaty, Lia D. ^{[3
]}

Achmad, Sjamsul A. ^{[3
]}

Hakim, Euis H. ^{[3
]}

Kaneda, Miyuki ^{[2
]}

Takahashi, Kunio ^{[1
]}

机构：

[1] Meiji Pharmaceut Univ, Dept Pharmacognosy & Phytochem, Kiyose, Tokyo 2048588, Japan

[2] Shujitsu Univ, Sch Pharm, Naka Ku, Okayama 7038516, Japan

[3] Bandung Inst Technol, Nat Prod Res Grp, Dept Chem, Bandung 40132, Indonesia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 15期

基金：

日本学术振兴会;

关键词：

beta-Secretase; BACE-1; Alzheimer; Amentoflavone; Biflavonoid; 2,3-Dihydroamentoflavone; 2,3-Dihydro-6-methylginkgetin; ALZHEIMERS-DISEASE; AMYLOID HYPOTHESIS; DENTICULATA; GINKGETIN;

D O I：

10.1016/j.bmcl.2010.06.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 mu M, respectively. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4558 / 4560

页数：3

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