Matrine is a component of the traditional Chinese medical herb Sophora flavescens Ait, which is widely used to treat diseases such as viral
hepatitis,
cardiac arrhythmia and skin
inflammations. As indicated by previous reports, the molecular mechanism of
matrine's anti-
cancer effect has been poorly clarified. In this study, we used both in vitro and in vivo models to investigate
matrine's antitumor effect and its possible molecular mechanisms. Murine
hepatocellular carcinoma H22 cells were cultured in the presence of
matrine at various concentrations (0.2 - 2.0 mg/mL). A dose-dependent antiproliferation effect was observed. The 50 % inhibitory concentration (IC (50)) was 0.6 mg/mL. Antiproliferation effects of
matrine were associated with an increase in cells arrested in the G (1) phase of the cell cycle. Morphological changes, flow cytometric analysis and expression of the proapoptotic
protein Bax indicated that this anticancer effect was mediated via apoptosis. In vivo antitumor efficacy was evaluated following S. C. inoculation of H22 cells in BALB/c mice.
Matrine administrated I. P. resulted in strong in vivo anticancer activity. Our results showed that seven doses of
matrine at 50 mg/kg/dose inhibited 60.7 % of
tumor growth. Transmission electron microscope (TEM) analysis and histoimmunochemical staining for Bcl-2 and Bax
proteins also indicated induction of apoptosis in
tumor tissues by
matrine. Taken together, our results demonstrate that
matrine possesses strong antitumor activities in vitro and in vivo. Inhibition of cell proliferation and induction of apoptosis are the likely mechanisms responsible for
matrine's antitumor activities.