发布时间：2025-04-30

论文名称：A New A431/Cell Membrane Chromatography–online–high performance liquid chromatography /mass spectrometry Method for Screening Anti-EGFR Antagonists from Radix Sophorae Flavescentis

发表刊物：J Chromatogr A

摘要：The intracellular kinase domains of epidermal growth factor receptor (EGFR) in some tumor cells such as human epidermal squamous cells (A431 cells) are an important target for drug discovery. We have developed a new A431/cell membrane chromatography (A431/CMC)-online-high performance liquid chromatography/mass spectrometry (HPLC/MS) method for screening EGFR antagonists from medicinal herbs such as traditional Chinese medicines (TCMs). In this study, A431 cells with high EGFR expression levels were used to prepare cell membrane stationary phase (CMSP) in an A431/CMC model. The retention fractions eluted from the CMSP column were enriched onto a ODS pre-column and then switched into an HPLC/MS system by combining a 10 port columns switching valve. The screening results found that oxymatrine and matrine from Radix sophorae flavescentis (RSF) were the targeted components which could act on EGFR in similar manner of gefitinib as a control drug. There was a good relationship of their inhibiting effects on EGFR secretion and A431 cell growth in vitro. This new A431/CMC-online-HPLC/MS method can be applied for screening EGFR antagonists from TCMs such as RSF. It will be a useful method for drug discovery with natural medicinal herbs as a leading compound resource.

合写作者：SC Wang, M Sun, H Du, YM Zhang, LC He

卷号：2010,1217

页面范围：5246-5252

是否译文：否

发表时间：2010-07-09