Radix salviae miltiorrhizae is a widely used traditional Chinese medicine, it is the root and rhizome of Salvia miltiorrhiza Bge and belongs to the family Labiatae. Many of its pharmacological effects have been reported in a previous study. In this study, a two-dimension online analytical method of epidermal growth factor receptor cell membrane chromatography combined with liquid chromatography/mass spectrometry was built for recognition, separation and identification of active components from traditional Chinese herb Radix salviae miltiorrhizae. Gefitinib was used as positive control, while atenolol, nicotine, and nimodipine were used as negative controls to investigate the selectivity of the EGFR/CMC column and system suitability of this online analytical method. Cryptotanshinone was screened from Radix salviae miltiorrhizae by this online analytical method. Through in vitro pharmacological trials, cryptotanshinone showed obvious and dose-dependent inhibition activity in the range 0.40 to 50.0 μM. Molecular docking assay showed that the cryptotanshinone binding region was in very good agreement with gefitinib. The EGFR/CMC-online-LC/MS two-dimension analytical method was demonstrated as an effective screening method that rapidly recognizes and enriches active components acting on the epidermal growth factor receptor from Radix salviae miltiorrhizae and separates and identifies them.
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