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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
Alternative Title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
Li F(李凤)1; Zhang YM(张艳梅)1; QIU DANYE1; Kang JW(康经武)1
2015
Source PublicationJ. Chromatogr. A
Volume1400Pages:117-123
AbstractA 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.
Subtype论文
Subject Area分析化学
DOI10.1016/j.chroma.2015.04.055
URL查看原文
Indexed BySCI
Language英语
WOS IDWOS:000356742500014
Citation statistics
Cited Times:12[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.sioc.ac.cn/handle/331003/39691
Collection分析化学研究室
Corresponding AuthorKang JW(康经武)
Affiliation1.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
Recommended Citation
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.
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