An antitumour lipopeptide biosurfactant purified from Bacillus natto TK-1 was able to inhibit the proliferation of MCF-7 human breast-cancer cells in a dose- and time-dependent manner. The activity of lactate dehydrogenase release showed no significant difference between MCF-7 cells treated with lipopeptide and untreated controls. The antitumour activity of the lipopeptide in MCF-7 cells was associated with cell apoptosis determined by typical morphological changes and sub-G(1) peak in cell growth-phase distribution. The cell cycle was arrested at G(2)/M phase. In addition, the caspase activity assay revealed that lipopeptide-induced apoptosis in MCF-7 cells was associated with caspase 3.