The antiproliferative activity and underlying mechanisms of jaspolide B, an isomalabaricane-type triterpene, isolated from the sponge Jaspis sp., were investigated using human promyeloleukemic HL-60 cells. Jaspolide B arrested HL-60 cells in the G2/M phase of the cell cycle and induced apoptosis of HL-60 cells in a dose- and time-dependent manner. Moreover, the poly (ADP-ribose) polymerase (PARP) protein was cleaved by jaspolide in a dose- and time-dependent way. Jaspolide B with an ICs0 value of 0.61 μmol/L was found to be comparable efficacy as that of paclitaxel (IC50:0.78 μmol/L). These results implicate the potential ofjaspolide B as a promising anticancer agent in chemotherapy of leukemia by arresting cell cycle progression at G2/M phase and triggering apoptosis.