Investigation of in vivo bioactive components and holistic quality control of Sarcandrae Herba

Sarcandrae Herba (SH) is a common traditional Chinese medicine (TCM) for the treatment of inflammation and immunity related diseases. However, the current various quality control for SH do not really associate with bioactive makers due to its in vivo bioactive components have not yet been fully addressed, so that a universal international quality control cannot be developed. In this research, an ultra-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UPLC/Q-TOF-MS) was adopted to describe the metabolic profiles after the oral administration of SH extract in rats and 24 prototype components and 26 metabolites were identified in biological samples of rats (plasma, urine, bile, feces). Then, peak area-time curves were adopted to preliminarily estimate the dynamic feature of 22 absorbed components in rat plasma and non-compartmental analysis (NCA) model were performed to calculate primary pharmacokinetic parameters by using WinNolin. Furthermore, a validated UPLC/Q-TOF-MS method was developed to study the plasma kinetics of the two bioactive and representative components (rosmarinic acid and isofraxidin) in rat plasma. Based on the in vivo bioactive components results, several components including coumarins, caffeoyl derivatives and flavonoids were selected as quality control components. Afterwards, a rapid identification method was established based on the Extractive Reference Substance (ERS), which covers the overall chemical profile of HPTLC for SH. A characteristic chromatogram containing principal components, anti-inflammatory active components and in vivo bioactive components as well as a Single Standard for Determination of Multiple components (SSDMC) method was developed and applied to the determination of six components of 38 batches of SH from 8 origins by UPLC. This study established a holistic quality control of SH on the basis of metabolic profiles and kinetics investigation, and it also proposed a strategy for the improvement of quality control for TCM based on the discovery of in vivo bioactive components.