Cell membrane-immobilized magnetic fluorescence nanoparticles as a screening platform for drug lead discovery.

Cell membrane biomimetic screening technology enables nanomaterials to have unique biointerface targeting function and is widely used in the field of drug lead compound discovery. Here, Coronary artery smooth muscle cell (CASMC) membrane camouflaged Nile Red-doped Polyethyleneimine (PEI) functionalized magnetic fluorescent nanomaterials (CMMFNPs) were synthesized based on the covalent coupling method and were employed for the enrichment and screening of anti-coronary heart disease active ingredients targeting CASMC from the Sanwei Tanxiang capsule. Various characterization tools confirmed the CMMFNPs were successfully prepared and possessed strong biocompatibility, good optical properties, magnetic properties and adsorption properties. Eventually, a total of six potential active ingredients were screened from the extract, and the pro-proliferative effects of the screened ligands on the CASMC were preliminarily evaluated by the cellular imaging assay. In addition, molecular docking demonstrated strong binding between these compounds and cell membrane receptors (CD36, AT1); CCK-8 and BrdU kits assay further validated from different perspectives that the screened ligands promoted cell proliferation in a concentration-dependent manner. In conclusion, this method combined the cell membrane bionic screening with cellular imaging, which could realize the rapid screening of active ingredients and at the same time evaluate the pharmacological activities of the screened ligands, is expected to provide an effective tool for the discovery of new drugs.