Schizandriside, a natural product isolated and purified from the leaves of Miconia rubiginosa with anti-inflammatory effect, shows significant cytotoxicity against A549, SK-OV-3, SK-MEL-2, and HCT-15 cell lines with inhibitory concentration (IC50) values of 3.26-8.89 uM, and has inhibitory activities against nitric oxide and prostaglandin E(2) production in IFN-γ- and lipopolysaccharide-stimulated RAW 264.7 cells.