An improved cell membrane chromatography method for the simultaneous screening of two epidermal growth factor receptor antagonists from radix scutellariae

作者：Sun, Meng; Hou, Xiaofang; Lin, Yuanyuan; Zhang, Jie; Wang, Sicen^*

来源：Journal of Separation Science, 2015, 38(18): 3145-3150.

DOI：10.1002/jssc.201500362

• Inhibitor
• Liquid chromatography
• Mass spectrometry
• Membrane receptor
• Radix Scutellariae

A high-expression epidermal growth factor receptor cell membrane chromatography using the silica gel with the average particle size of 3 mu m as the stationary phase carrier coupled with high-performance liquid chromatography and mass spectrometry was established for the online screening of epidermal growth factor receptor antagonists from Radix Scutellariae (Huang Qin in Chinese), a traditional Chinese medicine. In this study, the growth factor receptor cell membrane chromatography model using the smaller particle size carrier showed a higher efficiency for simultaneous screening baicalein, another one of the potential epidermal growth factor receptor antagonists from Radix Scutellariae extract besides wogonin, which was found in our previous work. The molecular docking result showed the occupancy site and binding mode of baicalein and wogonin with epidermal growth factor receptor tyrosine kinase were similar to gefitinib. The result of the assay for the in vitro inhibitory activity showed that baicalein and wogonin inhibited the growth of the high-expression epidermal growth factor receptor cell in a dose-dependent manner and even achieved a better inhibition effect than gifitinib in the low-dosage range.

• 出版日期2015-9
• 单位西安交通大学