Screening of Anti-EGFR Components from Aconitum Soongaricum Stapf. in Xinjiang Province Based on Cell Membrane Chromatography / 中国药师

ABSTRACT

Objective:To screen anti-EGFR components from Aconitum soongaricum Stapf. and investigate their inhibitory effect on HEK293 cells and EGFR/HEK293 high expression cell lines. Methods:A two-dimensional online system (EGFR/CMC-HPLC-MS) was built to screen anti-EGFR active compounds from Aconitum soongaricum Stapf.;molecular docking assay was performed to determine the binding affinity of the components to EGFR;MTT was used to confirm the inhibition effect of the screened compounds on HEK293 cells and EGFR/HEK293 high expression cell lines.Results:The screening results showed that aconitine,12-epi-napellin and songorine were the active components acting on EGFR like gefitinib; molecular docking assay showed the targeting components acting on EGFR in the similar manner with gefitinib used as a positive control drug; MTT assay confirmed the screened components had inhibitory effects on HEK293 cells and EGFR/HEK293 high expression cell lines in a dose-dependent manner within the dose range of 0.4- 50.0 μmol·L-1. Conclusion:The screening results are apparently consistent with the pharmacological effect. The online EGFR/CMC-HPLC-MS method has a good application prospect in the rapid screening of the active compounds in the complex system of traditional Chinese medicines,and fully demonstrates such advantages of cell membrane chromatography as simple and rapid with high efficiency.