Dioscin is a natural steroid saponin derived from several plants, showing the potent anti-cancer effect against a variety of tumor cell lines. Pharmacological studies have shown that dioscin processes anti-cerebral ischemia/reperfusion injury, anti-liver fibrosis and anti-obesity effects. Dioscin markedly inhibited cell viability, colony formation, motility and induced apoptosis in prostate cancer cells. Dioscin remarkably suppressed the migratory and invasive capacities of melanoma cells. In preclinical models, dioscin showed significant anti-metastatic effects and suppress the tumor cell malignancy.