Abstract

Background Scutellaria baicalensis is an important medicinal plant used in China. Several compounds have been extracted from S. baicalensis using modern techniques. Baicalin, an active ingredient of S. baicalensis, is widely used clinically. However, its clinical use is limited owing to poor oral bioavailability and intestinal absorption. Objectives To evaluate the anti-tumor effect of baicalin magnesium salt (BA-MG, a novel magnesium salt form of baicalin with superior water solubility) on the human hepatocellular carcinoma cell line, HepG2. Materials and Methods Seven groups were established, including three dosages of BA-MG (200, 250, and 300 µg/mL), baicalin, dimethyl sulfoxide (DMSO) (negative control), magnesium sulfate (negative control), and control groups. Cell proliferation was determined using the cell counting kit-8 (CCK-8) assay. Cell cycle and apoptosis were detected by flow cytometry. Cell migration was determined using a cell scratch assay. Protein expression was determined using western blotting. Results In vitro, BA-MG inhibited proliferation, reduced cell cloning and migration abilities, induced cell cycle arrest, and promoted apoptosis of HepG2 cells (all p < 0.05). The effects of baicalin and BA-MG on proliferation and migration, cell cycle, and apoptosis may be attributed to decreasing the expression of Bcl-2, ROCK-1, proliferating cell nuclear antigen (PCNA), and cyclin E, as well as increasing the expression of Bax and caspase-9. The efficacy of BA-MG is superior to that of baicalin at the same dose. Conclusion BA-MG showed superior effects on inhibiting cell proliferation and inducing apoptosis in liver cancer cells.

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