α-Hederin is a monosaccharide pentacyclic triterpene saponin compound derived from the Chinese herb, Pulsatilla. It has garnered considerable attention for its anti-tumor, anti-inflammatory, and spasmolytic pharmacological activities. Given the rising incidence of cancer and the pronounced adverse reactions associated with chemotherapy drugs—which profoundly impact the quality of life for cancer patients—there is an immediate need for safe and effective antitumor agents. Traditional drugs and their anticancer effects have become a focal point of research in recent years. Studies indicate that α-Hederin can hinder tumor cell proliferation and impede the advancement of various cancers, including breast, lung, colorectal, and liver cancers. The principal mechanism behind its anti-tumor activity involves inhibiting tumor cell proliferation, facilitating tumor cell apoptosis, and arresting the cell cycle process. Current evidence suggests that α-Hederin can exert its anti-tumor properties through diverse mechanisms, positioning it as a promising agent in anti-tumor therapy. However, a comprehensive literature search revealed a gap in the comprehensive understanding of α-Hederin. This paper aims to review the available literature on the anti-tumor mechanisms of α-Hederin, hoping to provide valuable insights for the clinical treatment of malignant tumors and the innovation of novel anti-tumor medications.