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Cancer represents a major global health threat, and the development of effective anticancer therapies is urgently needed. Sanguisorba officinalis (DY), a traditional Chinese herbal medicine, possesses properties including cooling blood and promoting blood circulation, detoxifying pathogenic toxins, and astringing sores. Increasing evidence suggests that DY and its bioactive constituents exhibit notable anti-tumor effects, with mechanisms that align with traditional Chinese medical principles of enhancing Zhengqi (fuzheng) and removing Xieqi (quxie). However, a comprehensive review that systematically summarizes the antitumor potential of DY and its bioactive constituents is still lacking. In this review, we summarize the anticancer effects of DY extracts and Ziyuglycosides. In vitro studies demonstrate that DY and its active components can inhibit tumor cell proliferation, induce cell cycle arrest, trigger mitochondria-mediated apoptosis, enhance autophagic flux, and suppress invasion and metastasis by regulating Wnt/β-catenin, PI3K/AKT/mTOR, MAPK, and EGFR/NF-κB signaling pathways, as well as downregulating epithelial-mesenchymal transition-related transcription factors and matrix metalloproteinases. In vivo studies confirms DY and its active components inhibit tumor growth and metastasis, regulate the tumor immune microenvironment, modulate Th17/Treg balance, activate CD8+ T cells, and enhance the anti-tumor immune responses. Notably, clinical application evidence indicates that Diyu Shengbai Pian, a preparation derived from DY, have been proven effective in alleviating leukopenia caused by chemotherapy or radiotherapy, highlighting DY's dual therapeutic potential in tumor suppression and mitigating treatment-related adverse reactions. However, current research mainly focuses on in vitro cellular studies and in vivo animal models, lacking large-scale, standardized clinical trials to validate its long-term efficacy and safety in humans. This review systematically summarizes the mechanisms of the anti-tumor and immunomodulatory effects of DY and its active components, and outlines advancements in improving their in vivo delivery efficiency, providing a theoretical basis and research reference for the translational application of DY in cancer therapy.