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Secondary plant metabolites are evolutionary-designed molecules that interact with multiple biological targets in human organisms. Identification of pharmacologically active phytochemicals is usually a time consuming and costly process. Cellular membrane affinity chromatography (CMAC) allows the detection of secondary metabolites present in complex natural matrices, e.g. plant extracts and their interactions with the immobilized fully-functional transmembrane proteins. After the isolation process of the binding compounds, CMAC columns can be used to study the binding process between the potential new ligands and the immobilized transmembrane protein target. The following parameters can be determined using CMAC columns: binding affinity (K d ), association rate constant (k on ), dissociation rate constant (k off ) and the equilibrium constant for complex formation (K). This review summarizes the preparation steps and the use of CMAC columns in the drug discovery process of new potential drug leads present in complex natural matrices.

Cellular membrane affinity chromatography (CMAC) in drug discovery from complex natural matrices