| Illuminating of constitutes, screening of bioactive components andestablishing of pharmacology in traditional Chinese medicines (TCMs) are thekey subjects for modernization of TCMs. High-throughput screening techniqueused in development of synthetic drugs does not meet the pharmacology of TCMson account of their multi-component, multi-target and combined effect in therapy.Whereas the facts, many new strategies have been developed for screeningconstitutes of TCMs in the past decades. In this thesis, the present state of the artof screening strategies for bioactive compounds in TCMs are summarized, it isindicated that the interaction between drugs and targets but changes in vivo weremostly focused.The metabolizing fingerprinting analysis of TCMs has been developed forpharmacological screening by rat liver homogenate in vitro. The method ofmetabolism in vitro has been estabolished by SD rat liver homogenate. Themetabolism of phenacetinum was investigated for availability. The diversity andcomparability about extracts of Cortex Phellodendri etc. was analyzed before andafter metabolism in vitro by means of chromatographic and MALDI-TOF-MSfingerprints.By means of the metabolism methods in vitro, antimicrobial activities,agglutination and antineoplastic activity were determined from the extracts,metabolites and components of Radix Salviac miltiorrhizae and Radix et RhizomaRhei by pharmacological assays in vitro. The changes of activities were causedfrom the metabolism of some components in TCMs, and the bioactivecomponents with metabolism activity were discovered simultaneously. An antineoplastic compound, coniferyl ferulate, was screened and identifiedfrom the extract of Rhizoma Chuanxiong by metabolism methods in vitro. Itsmetabolite was also identified as ferulic acid ethyl ester,and antineoplastic activityof this metabolite was not observed anymore. The proposed metabolism pathwayof coniferyl ferulate was illustrated in vitro.
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