Anticholinesterase, antioxidant, and beta-amyloid aggregation inhibitory constituents from Cremastra appendiculata

被引：0
作者：
Yanbei Tu
Jiwu Huang
Yanfang Li
机构：
[1] School of Chemical Engineering,
[2] Sichuan University,undefined
来源：
Medicinal Chemistry Research | 2018年 / 27卷
关键词：
Alzheimer’s disease; Phenanthrenes; Cholinesterase; Antioxidant activity; β-amyloid peptide aggregation;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
The tubers of Cremastra appendiculata (D. Don) Makino (Orchidaceae) are used in traditional Chinese medicine for the treatment of cancer and bacterial infections. Its 95% ethanol extract was found to display potent inhibitory activities on butyrylcholinesterase (BChE) (IC50 = 23.66 µg/mL) and β-amyloid peptide aggregation (74.09% at 100 μg/mL). Active ethyl acetate extract afforded one bibenzyl (1), four phenanthrenes (2–5), and one rotenoid (6) by a bioassay-guided isolation. Compounds 2, 3, and 5 exhibited potent BChE inhibitory effects with IC50 values of 19.66, 32.80, and 37.79 µM, respectively. Kinetic studies indicated that both 2 and 3 were mixed-type BChE inhibitors. Their strong binding affinities to BChE were further confirmed by fluorescence quenching analysis. Meanwhile, 2 and 3 showed the effective DPPH and ABTS radical scavenging activities (EC50 < 11 μM) and inhibition effect on β-amyloid peptide aggregation (64.49 and 29.50% at 20 μM, respectively), suggesting they could serve as multifunctional potential agents for AD drugs development. This paper revealed the potential medicinal and economic values of C. appendiculata and its chemical constituents in AD prevention/treatment.
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页码：857 / 863
页数：6
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