Cepharanthine is a biscoclaurine alkaloid extracted from S. cepharantha that is cationic and amphipathic and has been reported to decrease the fluidity of biological membranes. It exhibits antiparasitic, antimalarial, antiviral, anti-inflammatory, antimetastatic, and anticancer activities in various cell and animal models. Cepharanthine can decrease LPS-stimulated expression of TNF-α, IL-6, and IL-1β in macrophages and prevent the activation of NF-κB, ERK, JNK, and p38 MAPK. It has also been shown to inhibit cell and tumor growth, inducing G1 phase cell cycle arrest and apoptosis, and decreasing expression of STAT3, Bcl-xL, c-Myc, and cyclin D1 in osteosarcoma models.