TL;DR: This review summarizes the recent investigations regarding the anti-cancer activities and possible molecular targets of MT and OMT for cancer prevention and treatment in order to provide clues and references for further study.
Abstract: Matrine (MT) and oxymatrine (OMT), two kinds of alkaloid components found in the roots of Sophora species, have various pharmacological activities and are demonstrated to have anti-inflammatory, anti-allergic, anti-virus, anti-fibrotic, and cardiovascular protective effects. They are recently proved to have anti-cancer potentials, such as inhibiting cancer cell proliferation, inducing cell cycle arrest, accelerating apoptosis, restraining angiogenesis, inducing cell differentiation, inhibiting cancer metastasis and invasion, reversing multidrug resistance, and preventing or reducing chemotherapy- or radiotherapy-induced toxicity when combined with other chemotherapeutic drugs. In this review, we summarize the recent investigations regarding the anti-cancer activities and possible molecular targets of MT and OMT for cancer prevention and treatment in order to provide clues and references for further study.
TL;DR: Mechanistically, it is found that matrine ameliorated DOX-induced uncoupling protein 2 (UCP2) downregulation, and UCP2 inhibition by genipin could blunt the protective effect of matrine on DOx-induced oxidative stress and cardiomyocyte apoptosis, and it might be a promising therapeutic agent for the treatment of DOX -induced cardiotoxicity.
TL;DR: It is demonstrated that matrine exhibited a protective effect on LPS-induced acute lung injury by inhibiting of the inflammatory response, which may involve the suppression of ROS and tissue oxidative stress.
TL;DR: This review summarizes research developments of matrine and its derivatives as anticancer agents and suggests a few possible research directions, suggestions and clues for future work on the development of novel matrine-based anticancer agent with improved expected activities and lesser toxicity.
TL;DR: Inhibition of cell proliferation and induction of apoptosis are the likely mechanisms responsible for matrine's antitumor activities.
Abstract: 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.