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Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of humanacetylcholinesterase and butyrylcholinesterase
Wang,Yue-Hu1; Wan,Qin-Li2; Gu,Cheng-Ding3; Luo,Huai-Rong2; Long,Chun-Lin1,4
2012-09-08
发表期刊Chemistry Central Journal
ISSN1752-153X
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
语种英语
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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
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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).
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