Abstract
We describe a novel biomembrane affinity sample pretreatment technique to quickly screen and preconcentrate active components from traditional Chinese medicine (TCM), which adopts cell membrane coated silica particles (CMCSPs) as affinity ligands which benefit the biomembrane’s ability to maximize simulation of drug-receptor interactions in vivo. In this study, the prepared CMCSPs formed by irreversible adsorption of fibroblast growth factor receptor 4 (FGFR4) cell membrane on the surface of silica were characterized using different spectroscopic and imaging instruments. Drug binding experiments showed the excellent adsorption rate and adsorption capacity of FGFR4/CMCSPs compared with non-coated silica particles. The FGFR4/CMCSPs were used as solid-phase extraction sorbents to pretreat the TCM Aconitum szechenyianum Gay. The resultant FGFR4/CMCSPs exhibited good performance. In addition, high selectivity and recognition ability of the FGFR4/CMCSPs were determined by selectivity experiments. Four alkaloid were screened and identified, one of these alkaloid, napellonine, showed favorable anti-tumor activity in preliminary pharmacological verification trials including cell proliferation and molecular docking assays. The proposed cell membrane affinity sample pretreatment method is a reliable, effective and time-saving method for fast screening and enriching active compounds and can be extended to pretreat other TCMs as leading compounds resources.
Highlights
Solid-phase extraction (SPE)[1], a popular sample pretreatment technique, has been developed and widely used due to its high speed[2], availability[3, 4], simplicity[5, 6] and high preconcentration factors
We identified the other three retention components as 12-epinapelline, benzoylaconitine and 3-deoxyaconitine, respectively. These results demonstrated that the Fibroblast growth factors receptor 4 (FGFR4)/cell membrane coated silica particles (CMCSPs) SPE method had the ability to build a screening and enriching active components model from complicated samples
FGFR4/CMCSPs were successfully prepared using silica particles coated with FGFR4 cell membrane as selective affinity sorbents for screening and preconcentrating bioactive compounds from complex samples
Summary
Solid-phase extraction (SPE)[1], a popular sample pretreatment technique, has been developed and widely used due to its high speed[2], availability[3, 4], simplicity[5, 6] and high preconcentration factors. The cell membrane is an effective tool to investigate the action mechanism and screen active drugs[19, 20]. To this end, we designed novel cell membrane coated silica particles (CMCSPs) which recognized and preconcentrated bioactive compounds from traditional Chinese medicine (TCM). TCMs are natural therapeutic remedies and are attracting significant attention due to their clinical use and reliable treatment effects. They can be regarded as a source of leading compounds for new drug discovery[21, 22]. FGFR4 may be a potential drug target for screening anti-tumor leading compounds
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