Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of humanacetylcholinesterase and butyrylcholinesterase

doi:10.1186/1752-153X-6-96

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	Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of humanacetylcholinesterase and butyrylcholinesterase
	Wang,Yue-Hu 1; Wan,Qin-Li 2; Gu,Cheng-Ding 3; Luo,Huai-Rong2 ; Long,Chun-Lin 1,4
	2012-09-08
发表期刊	Chemistry Central Journal
ISSN	1752-153X
卷号	6 期号:1
摘要	AbstractBackgroundAlzheimer’s disease (AD) is a neurologically degenerative disorder that affects more than20 million people worldwide. The selective butyrylcholinesterase (BChE) inhibitors and bivalentcholinesterase (ChE) inhibitors represent new treatments for AD.FindingsA series of lycorine derivatives (1–10) were synthesized and evaluated foranti-cholinesterase activity. Result showed that the novel compound2-O-tert-butyldimethylsilyl-1-O-(methylthio)methyllycorine (7) wasa dual inhibitor of human acetylcholinesterase (hAChE) and butyrylcholinesterase (hBChE) withIC50 values of 11.40 ± 0.66 μM and 4.17 ± 0.29 μM, respectively. Thestructure-activity relationships indicated that (i) the 1-O-(methylthio)methyl substituentin lycorine was better than the 1-O-acetyl group for the inhibition of cholinesterase; (ii)the acylated or etherified derivatives of lycorine and lycorin-2-one were more potent against hBChEthan hAChE; and (iii) the oxidation of lycorine at C-2 decreases the activity.ConclusionAcylated or etherified derivatives of lycorine are potential dual inhibitors of hBChE and hAChE.Hence, further study on the modification of lycorine for ChE inhibition is necessary.
关键词	Amaryllidaceae alkaloids Lycorine Acetylcholinesterase Butyrylcholinesterase
DOI	10.1186/1752-153X-6-96
语种	英语
WOS记录号	BMC:10.1186/1752-153X-6-96
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/61813
专题	中国科学院昆明植物研究所
通讯作者	Wang,Yue-Hu; Long,Chun-Lin
作者单位	1.Kunming Institute of Botany, Chinese Academy of Sciences; Key Laboratory of Economic Plants and Biotechnology 2.Kunming Institute of Botany, Chinese Academy of Sciences; State Key Laboratory of Phytochemistry and Plant Resources in West China 3.Nanjing University; School of Chemistry and Chemical Engineering 4.Minzu University of China; College of Life and Environmental Sciences
推荐引用方式 GB/T 7714	Wang,Yue-Hu,Wan,Qin-Li,Gu,Cheng-Ding,et al. Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of humanacetylcholinesterase and butyrylcholinesterase[J]. Chemistry Central Journal,2012,6(1).
APA	Wang,Yue-Hu,Wan,Qin-Li,Gu,Cheng-Ding,Luo,Huai-Rong,&Long,Chun-Lin.(2012).Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of humanacetylcholinesterase and butyrylcholinesterase.Chemistry Central Journal,6(1).
MLA	Wang,Yue-Hu,et al."Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of humanacetylcholinesterase and butyrylcholinesterase".Chemistry Central Journal 6.1(2012).