Screening of epidermal growth factor receptor inhibitors in natural products by capillary electrophoresis combined with high performance liquid chromatography-tandem mass spectrometry

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	Screening of epidermal growth factor receptor inhibitors in natural products by capillary electrophoresis combined with high performance liquid chromatography-tandem mass spectrometry
	Li F(李凤)1; Zhang YM(张艳梅)1; QIU DANYE 1; Kang JW(康经武)1
刊名	J. Chromatogr. A
	2015
卷号	1400 页码:117-123
其他题名	毛细管电泳结合高效液相色谱-质谱联用用于天然产物中表皮生长因子受体抑制剂的筛选
通讯作者	康经武
英文摘要	A method for screening of inhibitors to epidermal growth factor receptor (EGFR) in natural product extracts with capillary electrophoresis (CE) in conjunction with high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) is reported. The method was established by employing 5-carboxyfluorescein labeled substrate peptide, two commercially available EGFR inhibitors OSI-744 and ZD1839, and a small chemical library consisted of 39 natural product extracts derived from the Traditional Chinese Medicines. Biochemical assay of crude natural product extracts was carried out by using CE equipped with a laser induced fluorescence detector. The CE separation allowed an accurately quantitative measurement of the phosphorylated product, hence the measurement of the enzymatic activity as well as the inhibition kinetics. The hits are identified if the peak area of the phosphorylated product is reduced in comparison with the negative control. The active constituents in the natural product extract were then identified by an assay-guided isolation with HPLC-MS/MS system. With the method, the flavonoids component of the Lycopus lucidus extract, namely quercetin and rutin were identified to be the active ingredients. Their IC50 values were determined as 0.88 mu M and 10.1 mu M, respectively. This result demonstrated a significant merit of our method in the identification of the bioactive compounds in natural products. (C) 2015 Elsevier B.V. All rights reserved.
学科主题	分析化学
收录类别	SCI
原文出处	http://dx.doi.org/10.1016/j.chroma.2015.04.055
语种	英语
WOS记录号	WOS:000356742500014
内容类型	期刊论文
源URL	[http://ir.sioc.ac.cn/handle/331003/39691]
专题	上海有机化学研究所_分析化学研究室
作者单位	1.中科院上海有机化学研究所, 生命有机化学国家重点实验室 2.上海科技大学
推荐引用方式 GB/T 7714	Li F,Zhang YM,QIU DANYE,et al. Screening of epidermal growth factor receptor inhibitors in natural products by capillary electrophoresis combined with high performance liquid chromatography-tandem mass spectrometry[J]. J. Chromatogr. A,2015,1400:117-123.
APA	李凤,张艳梅,QIU DANYE,&康经武.(2015).Screening of epidermal growth factor receptor inhibitors in natural products by capillary electrophoresis combined with high performance liquid chromatography-tandem mass spectrometry.J. Chromatogr. A,1400,117-123.
MLA	李凤,et al."Screening of epidermal growth factor receptor inhibitors in natural products by capillary electrophoresis combined with high performance liquid chromatography-tandem mass spectrometry".J. Chromatogr. A 1400(2015):117-123.