Abstract: Three triterpenes and two steroidal compounds were isolated from the dry root of Momordica dioica. Their structures were elucidated by spectral analyses(MS, IR,¹HNMR,¹³CNMR and DEPT) and chemical methods. These compounds are α-spinasterol octadecanonate(I), α-spinasterol-3-O-β-D-glucopyranoside(II), 3-O-β-D-glucuronopyranosyl gypsogenin(III), 3-O-β-D-glucopyranosyl gypsogenin(IV) and 3-O-β-D-glucopyranosyl hederagenin(V). Constituent III is a new compound.The CHCl₃ extract of Momordica dioica roots and five isolated constituents showed anticancer activity in pharmacologic testing on cancer cell(L₁₂₁₀). The growth inhibitory index(%) of compound II was shown to be 50%, at the dose of 4 μg·ml^-1.