STRUCTURE-ACTIVITY RELATIONSHIPS OF BIFLAVONOIDS FOR β-SECRETASE (BACE-1) INHIBITORY ACTIVITY

被引：8

作者：

Sasaki, Hiroaki ^{[1
]}

Kitoh, Yuki ^{[2
]}

Miki, Kazuhiko ^{[2
]}

Kinoshita, Kaoru ^{[2
]}

Koyama, Kiyotaka ^{[2
]}

Kaneda, Miyuki ^{[1
]}

Takahashi, Kunio ^{[2
]}

机构：

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

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

来源：

HETEROCYCLES | 2012年 / 85卷 / 11期

关键词：

Biflavonoid; Amentoflavone; BACE-1; beta-Secretase; Alzheimer's Disease;

D O I：

10.3987/COM-12-12561

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Bioactive natural products are useful sources of new pharmaceutics. Their analogues are also important for evaluating structure-activity relationships. In this study the structure-activity relationships of 2,3-dihydro-6-methylginketin (1) for BACE-1 inhibitory activity were studied. Biflavonoids consisting of flavanone and flavone, and also the presence of a methoxy group at the C-4' position, were found to be important for strong activity. 2,3-Dihydro-6-methylbilobetin (2) showed strong activity with an IC50 value of 0.56 mu M.

引用

页码：2749 / 2756

页数：8

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