Chemical Composition, Antitumor Activity, and Mechanisms of the Traditional Chinese Medicine Formulation Xiao-ai-ping

M. tenacissima has been traditionally used to treat a variety of diseases, including relieving cough and dyspnea, eliminating stasis, unblocking meridians, increasing lactation, clearing heat, and removing toxins. Currently, the chemical structures of 248 compounds from M. tenacissima have been identified, predominantly C21 steroids. Modern pharmacological studies have demonstrated that its extract, formulated as Xiao-ai-ping injection, capsule, or tablet, exhibits broad clinical efficacy against various cancers (e.g., liver, lung, gastric, colorectal) and often enhances the effectiveness of conventional chemotherapy and radiotherapy while reducing toxicity. This review provides an overview of the traditional medicinal uses of M. tenacissima, its phytochemistry, and the antitumor mechanisms of its herbal preparation, Xiao-ai-ping. It also discusses the limitations of current research and future perspectives (such as the early-stage status of pharmacokinetic and pharmacodynamic studies, insufficient clinical evidence with a lack of high-quality, large-sample, long-term randomized controlled trials, and an incomplete understanding of the multi-target mechanisms of Xiao-ai-ping), offering guidance for those dedicated to advancing the plant’s role in phytopharmaceuticals.