ABSTRACT
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.
Subject(s)
Humans , Antineoplastic Agents, Phytogenic , Pharmacology , Therapeutic Uses , Berberine , Pharmacology , Therapeutic Uses , Berberine Alkaloids , Pharmacology , Therapeutic Uses , Cell Death , Cisplatin , Pharmacology , Therapeutic Uses , Coptis , Chemistry , Drug Evaluation, Preclinical , Methods , Drugs, Chinese Herbal , Pharmacology , Therapeutic Uses , Electric Impedance , Hep G2 Cells , Hepatoblastoma , Drug Therapy , Inhibitory Concentration 50 , Liver Neoplasms , Drug Therapy , Phytotherapy , Rhizome , ChemistryABSTRACT
Objective: To establish the GC-MS fingerprints of volatile oil in crude, water-processed, and vinegar-processed Cyperi Rhizoma, and to capture the whole scope of the chemical constituents changing. Methods: The fingerprints of volatile oil in crude, water-processed, and vinegar-processed Cyperi Rhizoma were established by GC-MS. And the data were analyzed by chromatographic fingerprint similarity evaluation software for Chinese materia medica (Version A). Results: The similarities of each group were good, which indicated that the technology was stable and feasible. The crude group gained 52 common peaks, 28 as the water-processed group, and 53 as the vinegar-processed group. Meanwhile, 46 chemical components among the peaks above were identified in total. Comparing with the three groups, the kinds and contents of many components in each group were changed after processing. With the crude group as reference, the differences between the water-processed group and vinegar-processed group were contrastively analyzed before and after processing, and the Cyperi Rhizoma processed with vinegar could remain the chemical constitutions in its volatile oil better. Conclusion: Using vinegar as processing accessory is scientific and reasonable. Vinegar could play a role in protecting the compounds of volatile oil in Cyperi Rhizoma steadily.