Phytochemical investigation of the petroleum ether and methylene chloride extracts of the stems of Euphorbia tithymaloides L. (Euphorbiaceae) afforded the triterpenes friedelane-3β-ol, 3-oxo-friedelane, euphane-7, 24-diene, 3β-ol (butyrospermol), and euphane -7, 25-diene, 3, 24-β-diols in addition to the diterpene derivative 1 α, 13 β, 14 α-trihydroxy-3 β, 7 β-dibenzenzoyloxy-9 β, 15 β-diacetoxyjatropha-5, 11-E-diene and the phytosterol β-sitosterol. The structures of the isolated compounds were established depend on spectroscopic and chemical evidences. The petroleum ether, methylene chloride, and methanolic extracts of the stems of E. tithymaliodes L. were tested in vitro by determining their action on oxidative stress status of rat liver homogenate for their hepatoprotective activity in addition, the pet ether extract was tested in vivo for its hepatoprotective activity and diterpene derivative was tested in vitro for cytotoxic activity.