Department of Applied Chemistry, Faculty of Science and Engineering, Kinki University, Kowakae, Higashiosaka-shi, Osaka 577-8502, Japan.
Phytother Res. 2010 Apr;24(4):510-3. doi: 10.1002/ptr.2967.
In the course of screening antidementia agents from natural products, five beta-secretase (BACE1) inhibitors were isolated from the root extract of Angelica dahurica (Umbelliferae). They were identified as furanocoumarins, isoimperatorin (1), imperatorin (2), (+)-oxypeucedanin (3), (+)-byakangelicol (4) and (+)-byakangelicin (5). Among them, compounds 2 and 4 showed significant inhibitory activity against beta-secretase (BACE1) with IC(50) values of 91.8 +/- 7.5 and 104.9 +/- 2.4 microM, respectively. Compounds 1-5 inhibited BACE1 activity in a dose-dependent manner.
在从天然产物中筛选抗老年痴呆症药物的过程中，从白芷（伞形科）根提取物中分离出 5 种β-分泌酶（BACE1）抑制剂。它们被鉴定为呋喃香豆素，异茴芹素（1）、茴芹素（2）、（+）-氧化前胡素（3）、（+）-白当归脑（4）和（+）-白当归素（5）。其中，化合物 2 和 4 对β-分泌酶（BACE1）表现出显著的抑制活性，IC50 值分别为 91.8±7.5 和 104.9±2.4μM。化合物 1-5 以剂量依赖的方式抑制 BACE1 活性。
