Oridonin is a bioactive ent-kaurane diterpenoid isolated from the traditional Chinese medicinal herb *Rabdosia rubescens* (Donglingcao). It is a white crystalline powder with a molecular formula of C₂₀H₂₈O₆. This natural product is characterized by a unique 7,20-epoxy structure and multiple oxygen-containing functional groups. Extensive pharmacological studies have identified oridonin as a potent anti-cancer agent with a broad spectrum of activity. It exhibits significant inhibitory effects against various cancer cell lines, including those of breast, liver, lung, and colorectal cancers. Its mechanisms of action are multifaceted, involving the induction of cell cycle arrest, promotion of apoptosis through both intrinsic and extrinsic pathways, inhibition of angiogenesis, and modulation of key signaling pathways such as NF-κB, MAPK, and PI3K/Akt. Due to its promising efficacy and relatively low toxicity, oridonin is considered a valuable lead compound for the development of novel anti-tumor drugs and is actively investigated in preclinical and clinical research. Beyond its primary focus in oncology, oridonin also demonstrates notable anti-inflammatory, antibacterial, and neuroprotective properties. Its complex structure makes total chemical synthesis challenging, and it is primarily obtained through plant extraction and purification. Research continues to explore its structure-activity relationships and develop more potent derivatives.