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学科主题: 物理化学
题名: Label-free cell phenotypic profiling identifies pharmacologically active compounds in two traditional Chinese medicinal plants
作者: Zhang, Xiuli1;  Deng, Huayun2;  Xiao, Yuansheng1;  Xue, Xingya1;  Ferrie, Ann M.2;  Elizabeth Tran2;  Liang, Xinmiao1;  Fang, Ye2
通讯作者: 梁鑫淼 ;  Ye Fang
刊名: RSC ADVANCES
发表日期: 2014
DOI: 10.1039/c4ra03609c
卷: 4, 期:50, 页:26368-26377
收录类别: SCI
合作性质: 
文章类型: Article
部门归属: 18
项目归属: 1803
产权排名: 待补充
WOS标题词: Science & Technology ;  Physical Sciences
类目[WOS]: Chemistry, Multidisciplinary
资助者: 1,1
研究领域[WOS]: Chemistry
英文摘要: Traditional Chinese Medicines (TCMs) are widely used in clinical practice and natural products have been a rich resource for drug discovery. Identification of pharmacologically active chemical constituents is essential to the future of TCMs and natural product-based drug discovery. Here we report a label-free cell phenotypic profiling strategy to identify active fractions and compounds of two TCM plants including Paederia scandens (Lour.) Merri. (Jishiteng in Chinese) and Millettia pachyloba Drake (Duyuteng in Chinese), and to determine their mechanisms of action. The extracts of both plants were first fractionated to 160 fractions. Label-free cell phenotypic profiling afforded by a resonant waveguide grating biosensor in a microplate were then used to identify the active fractions acting at three different cell lines including A431, A549 and HT29. Mass spectroscopy-directed purification was then used to identify and purify active compounds. NMR and mass spectroscopy were used to determine the chemical structures of the active compounds, and pharmacological assays were used to elucidate their mechanisms of action. Using this strategy, we have discovered that both medicinal plants contain moderately high amount of niacin, an agonist for hydroxyl carboxylic acid receptor-2. Literature mining further suggests that the presence of niacin in Paederia scandens may be responsible for its antidyslipidemic effect found in clinic studies. This study demonstrates the potential of label-free cell phenotypic profiling for identifying active fractions and compounds of TCMs as well as elucidating their mechanisms of action.
关键词[WOS]: DYNAMIC MASS REDISTRIBUTION ;  ACID METHYL-ESTER ;  DRUG DISCOVERY ;  NATURAL-PRODUCTS ;  PAEDERIA-SCANDENS ;  NICOTINIC-ACID ;  BETA(2)-ADRENERGIC RECEPTOR ;  ANTINOCICEPTIVE ACTIVITY ;  OPTICAL BIOSENSOR ;  GPR35 AGONISTS
语种: 英语
原文出处: 查看原文
WOS记录号: WOS:000338434800048
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/119803
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Chinese Acad Sci, Dalian Inst Chem Phys, Key Lab Separat Sci Analyt Chem, Dalian 116023, Liaoning, Peoples R China
2.Corning Inc, Biochem Technol Sci & Technol Div, Corning, NY 14831 USA

Recommended Citation:
Zhang, Xiuli,Deng, Huayun,Xiao, Yuansheng,et al. Label-free cell phenotypic profiling identifies pharmacologically active compounds in two traditional Chinese medicinal plants[J]. RSC ADVANCES,2014,4(50):26368-26377.
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