| Alkaloid, coumarin, and lignan compounds, recognized as interesting and valuable biologically active phytochemicals, are shown to exert in vitro and in vivo remarkable anti-cancer, anti-inflammatory, anti-microbial, anti-fungal, anti-virus, reversal effect of multidrug resistance (MDR) on tumors, anti-HIV and antioxidant activity. They also have effect on the metabolism of endogenous and exogenous substances by inhibiting the activity of cytochrome (CYP) P450 enzyme. This paper has focused on the alkaloids, coumarins, lignans from herbal medicines, using the methods of multidimensional representation on chemical ingredients and biological activity for effective parts of them by modern chromatography and multiple techniques. The platform of high performance liquid chromatography-diode array detector-tandem mass spectrometry, comprehensive two-dimensional liquid chromatography, and pressurized capillary electrochromatography were established to represent the fingerprint chromatograms of chemical ingredients and quality control of herbal medicines on alkaloids from Plumula Nelumbinis, coumarins from Fructus Cnidii, lignans from Fructus Schisandrae, and coumarins from Angelica Dahurica. Monolithic affinity capillary electrochromatography immobilizingα1-acid glycoprotein or bovine serum albumin was also set up for alkaloid-protein interaction screening, representing the biological activity of them to the model proteins. The results of this thesis provided methodological examples and technique platforms for research on modernization for quality control of Chinese materia medica and metabolites of them.
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