<p>Natural drugs have the advantages of multi-pathway, multi-target, low toxicity, and high efficiency, which make them widely used and effective in anti-tumor therapy. Dioscin is a steroidal saponin compound that can be extracted from Dioscaceae plants. In recent years, it has been found that Dioscin has potent anti-tumor effects, can inhibit tumor cell proliferation, induce apoptosis and autophagy, inhibits tumor cell metastasis, reverses multidrug resistance, and increases sensitivity to anticancer drugs, and thus inhibit tumor progression. Meanwhile, the construction of Dioscin nanocarriers can improve the efficiency of drug use, reduce drug toxicity, realize the precise delivery of drugs, and improve the bioavailability of Dioscin. In this paper, the anticancer mechanism and targets of Dioscin in recent years were reviewed, thereby providing new ideas and a theoretical basis for further research and promotion of Dioscin.</p> Graphical Abstract <p></p>