Sanguinarine is a benzophenanthridine alkaloid primarily isolated from plants of the Papaveraceae family, such as *Sanguinaria canadensis* (bloodroot) and *Chelidonium majus* (greater celandine). It is a quaternary ammonium salt with a planar, polycyclic aromatic structure, which contributes to its ability to intercalate into DNA and interact with various cellular targets. Its primary and most researched application is in the field of medicine, particularly as a potential anti-cancer agent. Sanguinarine exhibits a broad spectrum of pharmacological activities, including potent antiproliferative, pro-apoptotic, anti-angiogenic, and anti-metastatic effects against various cancer cell lines. The mechanisms involve induction of reactive oxygen species (ROS), cell cycle arrest, modulation of key signaling pathways (e.g., NF-κB, MAPK), and inhibition of topoisomerase enzymes. Beyond oncology, it has been studied for its antimicrobial, anti-inflammatory, and cardiovascular properties. Due to its natural origin and significant bioactivity, sanguinarine is classified as a bioactive natural product and a lead compound for drug development. It is also used in some dental hygiene products for its anti-plaque and anti-gingivitis effects. However, its clinical application is limited by potential toxicity at higher doses, necessitating further research into its safety profile and delivery systems.