期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 -, 页码 299-312出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.02.014
关键词
7,8-Dehydrorutaecarpine derivatives; Alzheimer's disease; Acetylcholinesterase; A beta aggregation; Antioxidant; Metal-chelating
资金
- Natural Science Foundation of China [81273433, 21172272]
- Specialized Research Fund for the Doctoral Program of Higher Education [20110171110051]
A series of 7,8-dehydrorutaecarpine derivatives were synthesized and characterized as potential multifunctional agents for treatment of Alzheimer's disease (AD). All of these synthetic compounds showed high acetylcholinesterase (AChE) inhibitory activity with IC50 values ranged from 0.60 to 196.7 nM, and good selectivity for AChE over butyrylcholinesterase (BuChE) (125- to 3225-fold). A Lineweaver-Burk plot and molecular modeling study indicated these compounds could bind to both catalytic active site and the peripheral anionic site of AChE. Besides, compounds showed higher activity of inhibiting AChE-induced amyloid-beta (A beta) aggregation than curcumin, higher anti-oxidative activity than Trolox, and could also be good metal chelators. Considering their low cytotoxicity, our results indicated that these derivatives provide good templates for developing new multifunctional agents for AD treatment. (C) 2013 Elsevier Masson SAS. All rights reserved.
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