School of Pharmacy, Shujitsu University, Naka-ku, Okayama 703-8516, Japan.
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4558-60. doi: 10.1016/j.bmcl.2010.06.021. Epub 2010 Jun 8.
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.
在这里，我们描述了一种amentoflavone 型二氢黄酮，它们从天然来源中分离出来，并被发现能抑制β-分泌酶（BACE-1）。研究了构效关系，化合物 1-8、10、17 和 18 表现出 BACE-1 抑制活性。在这些化合物中，2,3-二氢amentoflavone 17 和 2,3-二氢-6-甲基银杏黄酮 18 表现出较强的抑制作用，IC50 值分别为 0.75 和 0.35 μM。
