Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of humanacetylcholinesterase and butyrylcholinesterase
文献类型：期刊论文
| 作者 | Wang,Yue-Hu1; Wan,Qin-Li2; Gu,Cheng-Ding3; Luo,Huai-Rong2 ; Long,Chun-Lin1,4
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| 刊名 | Chemistry Central Journal
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| 出版日期 | 2012-09-08 |
| 卷号 | 6期号:1 |
| 关键词 | Amaryllidaceae alkaloids Lycorine Acetylcholinesterase Butyrylcholinesterase |
| ISSN号 | 1752-153X |
| DOI | 10.1186/1752-153X-6-96 |
| 英文摘要 | 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. |
| 语种 | 英语 |
| WOS记录号 | BMC:10.1186/1752-153X-6-96 |
| 出版者 | Springer International Publishing |
| 源URL | [http://ir.kib.ac.cn/handle/151853/61812]  |
| 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). |
入库方式： OAI收割
来源：昆明植物研究所
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