Breviscapine-induced apoptosis of human hepatocellular carcinoma cell line HepG2 was involved in its antitumor activity.

Breviscapine is a flavonoid constituent isolated from a traditional Chinese herb Erigerin breviscapus (Vant.) Hand-Mazz. To investigate the apoptosis-inducing effect of breviscapine on human hepatocellular carcinoma cell line HepG2 and explore the relative molecular mechanisms. HepG2 cells were treated with breviscapine at different concentrations and the inhibitory rate was analyzed by MTT assay. The morphological changes in cells were observed under an inverted light microscope and a fluorescence microscope and the apoptosis rate were detected by flow cytometry. Western blot was used to evaluate the protein expression. The viability of HepG2 cells was markedly inhibited in a concentration-dependent manner and obvious morphological changes were confirmed, including condensed chromatin and reduction in volume. The increased percentage of apoptotic cells was displayed by flow cytometry and the altered expression level of several apoptosis-associated proteins, Bcl-2, Bax and caspase-3, was detected by western blot. It is first discovered that breviscapine exhibited potential antitumor activity, induces remarkable apoptosis in HepG2 cells and promises to be a new candidate in future cancer therapy. Copyright (C) 2010 John Wiley & Sons, Ltd.