Abstract: Malignant tumors are a major chronic disease that poses a serious threat to human health. Surgical resection combined with drug assisted therapy is the main method of anti-tumor treatment, but nowadays, many anti-tumor drugs have drug resistance and adverse reactions. With the increasing incidence rate of tumors in recent years, the treatment of tumors with safe and effective traditional Chinese medicine has become a hot spot. Tripterygium wilfordii is a traditional Chinese medicine in China, which has been proven to have significant therapeutic effects on various malignant tumors. Among the active ingredients, the terpenoid compounds triptolide and celastrol are considered representative drugs for traditional Chinese medicine in treating tumors. This article comprehensively elaborated on the anti-tumor mechanism of terpenoids from Tripterygium wilfordii, and analyzed and expanded their combined therapy, in order to provide theoretical basis and research ideas for the in-depth research and clinical application of terpenoids from Tripterygium wilfordii.