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Planta Med 2008; 74(5): 540-545
DOI: 10.1055/s-2008-1074496
Natural Products Chemistry
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

BACE1 (β-Secretase) Inhibitory Chromone Glycosides from Aloe vera and Aloe nobilis

Liang Lv1 , 2 [*] , Qing-Yun Yang1 , 2 [*] , Ying Zhao1 , 2 , Chun-Suo Yao1 , 2 , Yang Sun2 , Eun-Ju Yang3 , Kyung-Sik Song3 , Inhee Mook-Jung4 , Wei-Shuo Fang1 , 2
  • 1Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine (Peking Union Medical College), Ministry of Education, Beijing, P. R. China
  • 2Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, P. R. China
  • 3School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University, Daegu, Korea
  • 4Department of Biochemistry, College of Medicine, Seoul National University, Seoul, Korea
Further Information

Publication History

Received: November 11, 2007 Revised: February 25, 2008

Accepted: February 27, 2008

Publication Date:
07 April 2008 (online)

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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 (β-secretase) with IC50 values of 39.0 and 20.5 × 10-6 M, as well as inhibition of Aβ1 - 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.

Key words

Aloe vera - Aloe nobilis - Liliaceae - chromone glycosides - BACE1 (β-secretase) inhibitor - Alzheimer’s disease (AD)

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1 Equal contributions to this work.

Prof. Wei-Shuo Fang

Institute of Materia Medica

Chinese Academy of Medical Sciences & Peking UnionMedical College

No. 1 Xiannongtan Street

Beijing 100050

People’s Republic of China

Phone: +86-010-6316-5229

Email: wfang@imm.ac.cn