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■ Structure-Activity Relationships of Biflavonoids for β-Secretase (BACE-1) Inhibitory Activity

Hiroaki Sasaki, Yuki Kitoh, Kazuhiko Miki, Kaoru Kinoshita, Kiyotaka Koyama, Miyuki Kaneda, and Kunio Takahashi*

*Department of Pharmacognosy and Phytochemistry, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose, Tokyo 204-8588, Japan

Abstract

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 μM.