Simultaneous screening of four epidermal growth factor receptor antagonists from C urcuma longa via cell membrane chromatography online coupled with HPLC–MS

The epidermal growth factor receptors ( EGFR s) are significant targets for screening active compounds. In this work, an analytical method was established for rapid screening, separation, and identification of EGFR s antagonists from Curcuma longa . Human embryonic kidney 293 cells with a steadily high expression of EGFR s were used to prepare the cell membrane stationary phase in a cell membrane chromatography model for screening active compounds. Separation and identification of the retention chromatographic peaks was achieved by HPLC – MS . The active sites, docking extents and inhibitory effects of the active compounds were also demonstrated. The screening result found that ar‐turmerone, curcumin, demethoxycurcumin, and bisdemethoxycurcumin from C urcuma longa could be active components in a similar manner to gefitinib. Biological trials showed that all of four compounds can inhibit EGFR s protein secretion and cell growth in a dose‐dependent manner, and downregulate the phosphorylation of EGFR s. This analytical method demonstrated fast and effective characteristics for screening, separation and identification of the active compounds from a complex system and should be useful for drug discovery with natural medicinal herbs.