Abstract: AIMTo study the anticancer effects of two novel highly oxygenated bisabolance sesquiterpene compounds from Cremanthodium discoideum Maxim on the human hepatoma cell line SMMC-7721. METHODSin vitro, the cytotoxity of compound 1, 2 was tested by MTT colorimetric assay, and the single-cell gel electrophoresis (SCGE) assay was used for assessing the DNA damage of SMMC-7721 cells induced by compound 1, 2. The apoptotic rate of SMMC-7721 cells was assayed by flow cytometry. RESULTSThe IC₅₀ of SMMC-7721 cells exposed to the two compounds for 72 h were (37±7) μg·mL^-1 and (22±9) μg·mL^-1, respectively. The result of SCGE showed that the two compounds (2, 4 and 8 μg·mL^-1, 48 h) were able to induce DNA damage in SMMC-7721 cells and showed dose-dependent effect. Flow cytometric analyses showed that after exposure to the two compounds for 48 h induced the apoptosis in SMMC-7721 cells. CONCLUSIONThe two novel highly oxygenated bisabolance sesquiterpene compounds showed significant inhibition effect on the growth of SMMC-7721 cells and its mechanism was probably related with the DNA damage and apoptosis induced by them.