AIM: To investigate the cytotoxic effects of the six protoberberine alkaloids(PAs) from Rhizoma Coptidis on HepG2 cells. METHOD: A systematic screening was conducted to investigate the dynamic response of HepG2 cells to the PAs using the impedance-based xCELLigence system. Cisplatin was selected as the positive control. The real time, concentration-response curves and the 50% inhibitory concentrations(IC50) were acquired to evaluate the anticancer activity of the PAs. RESULTS: All of the six PAs inhibited cell growth and induce death in HepG2 cells in a time- and concentration-dependent manner. The IC50 values of cisplatin, berberine, columbamine, coptisine, epiberberine, jatrorrhizine, and palmatine were 5.13, 42.33, 226.54, 36.90, 302.72, 383.54, and 456.96 μg·mL-1, respectively. The results obtained using the xCELLigence system corresponded well with those of the conventional methods. CONCLUSION: The xCELLigence system is a reliable and efficient tool for real-time screening of the cytotoxic effect of compounds in cell-based in vitro assays. Coptisine and berberine, with methylenedioxy group at C2 and C3 on the phenyl ring showed stronger effect.than the other four PAs. However, compared with cisplatin, the six PAs didn't show obvious cytotoxic effect on HepG2 cells.These results provided some useful data for the evaluation of the anticancer compounds, and the clinical application of traditional Chinese medicine.
Most of herbal medicines of different sources are used for the same treatment goal in clinic despite their tremendous differences of the quality.Because the clinical efficacy is closely related to the quality of medicines,the implementation of an effective quality control(QC)process is vital.Chemical methods based on content determination and chromatographic fingerprints(CFs)have been recommended as powerful tools.In spite of advances in QC,it is still difficult to determine that which of the chemical compositions can best reflect the correlation with the desired biological activity.Herein,we have focused on the biological activities of multi-source herbal medicines to establish an analytical method.By looking for correlations between the biological activities and their chemical compositions,the method can identify reasonable chemical indicators or chemical methods with biological activity information.In this study,high-performance liquid chromatography(HPLC)and microcalorimetry are combined as a useful method for evaluating the quality of Rhizoma coptidis from different sources.The results of biological fingerprints(BFs)showed that the antibacterial activity sequence of R.coptidis of different sources was Coptis teeta Wall.(CT)>Coptis chinensis Franch.(CC)>Coptis deltoidea C.Y.Cheng et Hsiao(CD).The"spectrum-activity"relationships between CFs and BFs were investigated using the canonical correlation analysis(CCA).Compared with the CCA result of CFs and BFs,the canonical correlation coefficient r1and r2were 0.9974 and 0.9752,respectively.It revealed that there are a close correlation between the spectrum-activity relationships and several of the major anti-bacterial components in the CFs,including jatrorrhizine,coptisine,palmatine,and berberine.Of course,R.coptidis was only a representative of multisource medical plants.The result of the current study will provide an effective reference for evaluating the quality of multisource herbal medicines.
LI JunXianYAN DanMA LiNaXIONG YinYAN ChunXiaLI BaoCaiPENG ChengXIAO XiaoHe
