来自库拉索芦荟和翠叶芦荟的β-分泌酶1（BACE1）抑制性色酮糖苷。

BACE1 (beta-secretase) inhibitory chromone glycosides from Aloe vera and Aloe nobilis.

作者信息

Lv Liang, Yang Qing-Yun, Zhao Ying, Yao Chun-Suo, Sun Yang, Yang Eun-Ju, Song Kyung-Sik, Mook-Jung Inhee, Fang Wei-Shuo

机构信息

Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine (Peking Union Medical College), Ministry of Education, Beijing, P. R. China.

出版信息

Planta Med. 2008 Apr;74(5):540-5. doi: 10.1055/s-2008-1074496.

DOI:10.1055/s-2008-1074496

PMID:18543151

Abstract

Four new chromone glycosides allo-aloeresin D (2) , C-2'-decoumaroyl-aloeresin G (8), 2'-O-coumaroyl-(S)-aloesinol (9), 2'-O-[ P-methoxy-(E)-cinnamoyl]-(S)-aloesinol (10) and nine known chromone glycosides ( 1, 3 - 7, 11 - 13) were isolated from two Aloe spp. plants, A. vera and A. nobilis. Among them, 1 and 8 showed significant inhibitory activity against BACE1 (beta-secretase) with IC (50) values of 39.0 and 20.5 x 10 (-6) M, as well as inhibition of Abeta (1-42) production by 7.4 and 12.3 %, respectively, in B103 neuroblastoma cells at 30 ppm. The preliminary structure-activity relationships of ALOE chromone glucosides were also discussed.

摘要

从两种芦荟属植物，即库拉索芦荟和斑纹芦荟中分离出了4种新的色酮糖苷，别芦荟树脂D（2）、C-2'-去香豆酰芦荟树脂G（8）、2'-O-香豆酰-（S）-芦荟醇（9）、2'-O-[对甲氧基-（E）-肉桂酰]-（S）-芦荟醇（10）以及9种已知的色酮糖苷（1、3 - 7、11 - 13）。其中，1和8对β-分泌酶（BACE1）表现出显著的抑制活性，IC（50）值分别为39.0和20.5×10（-6）M，并且在30 ppm时，对B103神经母细胞瘤细胞中β淀粉样蛋白（1-42）的产生分别抑制了7.4%和12.3%。还讨论了芦荟色酮糖苷的初步构效关系。