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学科主题: 药学
题名:
Synthetic phenylethanoid glycoside derivatives as potent neuroprotective agents
作者: Liu, Ying-Guo1; Li, Xiaxi1; Xiong, De-Cai1; Yu, Binhan1; Pu, Xiaoping1; Ye, Xin-Shan1,2
关键词: Phenylethanoid glycoside ; Neuroprotective agent ; Structure modification ; Antioxidant ; Anti-apoptosis
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2015-05-05
DOI: 10.1016/j.ejmech.2015.03.038
卷: 95, 页:313-323
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: NEURONAL PC12 CELLS ; RADICAL SCAVENGER ; OXIDATIVE STRESS ; SIALIC-ACID ; 1-METHYL-4-PHENYLPYRIDINIUM ION ; PHENYLPROPANOID GLYCOSIDES ; NEURODEGENERATIVE DISEASE ; OLIGOSACCHARIDE SYNTHESIS ; BIOLOGICAL EVALUATION ; INDUCED APOPTOSIS
英文摘要:

Several phenylethanoid glycoside derivatives were designed and synthesized. Most of the synthetic compounds showed significant neuroprotective effects, including antioxidative and anti-apoptotic properties. Specifically, target compounds displayed potent effects against various toxicities such as H2O2 and 6-hydroxydopamine (6-OHDA) in PCl2 cells. Among the synthetic derivatives, three compounds (5, 6, 8) exhibited much superior activities to the marketed drug Edaravone. The compounds were able to prevent the 6-OHDA-induced damage in PCl2 cells in a dose-dependent manner. The antiapoptotic effects could be observed via cell morphological changes. Moreover, the compounds significantly reduced the intracellular ROS increase resulting from 6-OHDA treatment. The preliminary structure activity relationships were also explored. Compounds 5, 6, 8 may hold the potential as promising neuroprotective agents and new lead compounds for the treatment of neurodegenerative diseases or cerebral ischemia. (C) 2015 Elsevier Masson SAS. All rights reserved.

语种: 英语
所属项目编号: 2012CB822100 ; 2013CB910700 ; 2012ZX09502001-001 ; 2012ZX09103301-048 ; 2012ZX09103201-042 ; 21232002
项目资助者: Ministry of Science and Technology of China ; National Natural Science Foundation of China
WOS记录号: WOS:000354139900027
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/61409
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Jiangxi Normal Univ, Natl Engn Res Ctr Carbohydrate Synth, Nanchang 330022, Jiangxi, Peoples R China

Recommended Citation:
Liu, Ying-Guo,Li, Xiaxi,Xiong, De-Cai,et al. Synthetic phenylethanoid glycoside derivatives as potent neuroprotective agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2015,95:313-323.
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