Lupeol is a triterpene that displays neuromodulatory, anti-hyperuricemic, anti-inflammatory, antioxidative, and anticancer chemotherapeutic activities. It inhibits tyrosinase oxidation of L-DOPA in the brain. It also decreases monosodium urate crystal-induced paw edema in animal models, indicating potential benefit as a treatment for gouty arthritis. In vitro, it decreases production of NO, decreases levels of iNOS and cyclooxygenase (COX-2) and also prevents generation of ROS by tert-butylhydroperoxide (t-BHP). Lupeol decreases free radical-mediated damage in animal models. It also exhibits anticancer benefit by inhibiting androgen-induced androgen receptor (AR) activity and prostate-specific antigen (PSA) expression; it competitively inhibits the androgen receptor and inhibits tumorigenicity of prostate cancer cells in vivo. Additionally, this compound decreases β-catenin levels, expression of matrix metalloproteinase 2 (MMP2), and activation of T cell factor responsive element in vitro.