The invention provides the application of an ophiopogonin compound in the preparation of drugs for preventing and treating tumors, wherein the tumor is a benign tumor or a malignant tumor, and the malignant tumor is selected from one or more of lung cancer, liver cancer, stomach cancer, breast cancer, colon cancer, leukemia, multiple myeloma, lymphoma, malignant melanoma, myeloproliferative disease solid tumor or hematological malignant tumor. The invention also provides an anti-tumor pharmaceutical composition, which contains a therapeutically effective amount of the compound shown in the formula (I) or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. As a compound capable of remarkably inhibiting tumor cell proliferation, the compound shown in the formula (I) or the pharmaceutically acceptable salt thereof has the advantages of small potential toxic and side effects, remarkable inhibition of tumor cell proliferation, broad-spectrum cancer resistance, easiness in preparation, low cost and the like, and has a wide anti-tumor application prospect clinically.