Glycoalkaloids is one of the main constituents of Solanum nigrum L., including solamargine, solasonine, and solanine. Glycoalkaloids was proved to have anti-cancer effects against lung cancer, breast cancer, liver cancer, pancreatic cancer, colorectal cancer, cervical cancer, prostate cancer, leukemia and other malignancies. Glycoalkaloids can inhibit cell proliferation, induce apoptosis and autophagy, block cell cycle, enhance effects of chemotherapy, inhibit epithelial-mesenchymal transition, metastasis and angiogenesis. These studies provide new basis for rational application and development of Glycoalkaloids.