Cudratricusxanthone A has potent anti-proliferative, antioxidative, and monoamine oxidase inhibitory effects, it also possesses anti-cancer activities and provide a basis for developing effective therapeutic agents to inhibit growth and metastasis of breast cancer. Cudratricusxanthone A inhibits lipopolysaccharide-induced neuroinflammation through inhibition of NF-κB and p38 MAPK pathways in BV2 microglia. Cudratricusxanthone A has antiplatelet, anticoagulant, and profibrinolytic activities, it reversibly inhibits CYP1A2, 2C8, and 2C9. It also exhibits the significant hepatoprotective effect on nitrofurantoin-induced cytotoxicity in human liver-derived Hep G2 cells.