beta-secretase inhibitory effects of furanocoumarins from the root of Angelica dahurica.
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.
Marumoto
Shinsuke
S
Department of Applied Chemistry, Faculty of Science and Engineering, Kinki University, Kowakae, Higashiosaka-shi, Osaka 577-8502, Japan.
Miyazawa
Mitsuo
M
D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D029969:Angelica / Q000737:chemistry*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D004353:Drug Evaluation, Preclinical; D011564:Furocoumarins / Q000302:isolation & purification / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry
D011564:Furocoumarins; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human