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Simultaneous screening of four epidermal growth factor receptor antagonists from C urcuma longa via cell membrane chromatography online coupled with HPLC–MS
Author(s) -
Sun Meng,
Ma Weina,
Guo Ying,
Hu Zhigang,
He Langchong
Publication year - 2013
Publication title -
journal of separation science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.72
H-Index - 102
eISSN - 1615-9314
pISSN - 1615-9306
DOI - 10.1002/jssc.201200961
Subject(s) - chemistry , epidermal growth factor receptor , chromatography , curcuma , gefitinib , high performance liquid chromatography , curcumin , cell growth , biological activity , active ingredient , membrane , epidermal growth factor , docking (animal) , virtual screening , drug discovery , receptor , biochemistry , pharmacology , in vitro , biology , paleontology , medicine , nursing
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.