triterpenoid saponins are glycosides with remarkable structural and bioactive diversity. They are becoming increasingly significant in the treatment of cancer due to their efficacy and safety. This chapter provides an update on the sources, pharmacological effects, structure-activity relationships, and clinical studies of anticancer triterpenoid saponins with a particular focus on the molecular mechanisms underlying their therapeutic properties. The correlative references and study reports described were collected through PubMed. The anticancer triterpenoid saponins enable the inhibition of cancer formation and progression by modulating multiple signaling targets related to cellular proliferation, apoptosis, autophagy, metastasis, angiogenesis, inflammation, oxidative stress, multidrug resistance, cancer stem cells, and microRNAs. This review provides new insights into the molecular basis of triterpenoid saponins in the chemoprevention and chemotherapy of cancer.
