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基于 A431 细胞膜色谱和在线高效液相色谱/质谱联用技术的蛇床子总生物碱作用于人表皮生长因子受体的活性成分筛选方法

A combined A431 cell membrane chromatography and online high performance liquid chromatography/mass spectrometry method for screening compounds from total alkaloid of Radix Caulophylli acting on the human EGFR.

机构信息

Key Laboratory of Environment and Genes Related to Diseases, Ministry of Education, China.

出版信息

J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Oct 15;878(28):2712-8. doi: 10.1016/j.jchromb.2010.08.010. Epub 2010 Aug 19.

Abstract

We have developed an online analytical method that combines A431 cell membrane chromatography (A431/CMC) with high performance liquid chromatography and mass spectrometry (LC/MS) for identifying active components from Radix Caulophylli acting on human EGFR. Retention fractions on A431/CMC model were captured onto an enrichment column and the components were directly analyzed by combining a 10-port column switcher with an LC/MS system for separation and preliminary identification. Using Sorafenib tosylate as a positive control, taspine and caulophine from Radix Caulophylli were identified as the active molecules which could act on the EGFR. This A431/CMC-online-LC/MS method can be applied for screening active components acting on EGFR from traditional Chinese medicines exemplified by Radix Caulophylli and will be of great utility in drug discovery using natural medicinal herbs as a source of novel compounds.

摘要

我们开发了一种在线分析方法,将 A431 细胞膜色谱(A431/CMC)与高效液相色谱和质谱(LC/MS)相结合,用于鉴定作用于人类 EGFR 的华西鬼臼活性成分。在 A431/CMC 模型上的保留分数被捕获到富集柱上,并通过结合 10 端口柱切换器与 LC/MS 系统进行分离和初步鉴定,直接对成分进行分析。以甲苯磺酸索拉非尼为阳性对照,华西鬼臼中的檗皮碱和华西鬼臼碱被鉴定为能够作用于 EGFR 的活性分子。这种 A431/CMC-在线-LC/MS 方法可用于从华西鬼臼等中药中筛选作用于 EGFR 的活性成分,对于以天然草药为来源的新型化合物的药物发现将非常有用。

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