Cepharanthine is an alkaloid found in Stephania that exhibits anti-parasitic, antimalarial, antiviral, anti-inflammatory, anti-metastatic, and anticancer chemotherapeutic activities. Cepharanthine inhibits the development of Plasmodium in vitro and inhibits cell fusion and entry of HIV-1 by decreasing plasma membrane fluidity. Additionally, cepharanthine decreases LPS-stimulated expression of TNF-α, IL-6, and IL-1β in macrophages and prevents the activation of NF-κB, ERK, JNK, and p38 MAPK; in animal models of lung injury, it decreases inflammation. This compound also inhibits cell and tumor growth, induces G1 phase cell cycle arrest and apoptosis, and decreases expression of STAT3, Bcl-xl, c-Myc, and cyclin D1 in osteosarcoma models. In models of cholangiocarcinoma, cepharanthine inhibits cell migration and tumor growth.