Abstract
To clarify whether the seeds of Croton macrostachyus can induce apoptosis, its methanolic extract was first subjected to a clonogenic survival assay, which measures long-term cytotoxic effects. Since it showed cytotoxicity on HCT116 human colon cancer cell lines, further separation was performed, and two single diterpene compounds were obtained. One of them was identified to be a novel compound, methyl 2-(furan-3-yl)-6a,10b-dimethyl-4-oxo-2,4,4a,5,6,6a,10a,10b-octahydro-1H-benzo[f]isochromene-7-carboxylate, based on the interpretation of the nuclear magnetic resonance spectroscopic and mass spectrometric data. Its treatment of HCT116 cells with 50 μg/mL triggered the cleavage of both initiator caspase-9 and effector caspase-7. Moreover, the cleavage of poly (ADP-ribose) polymerase, a substrate of caspase-7, increased after 24 h of treatment. These results demonstrate that this compound exerts antitumor activity by triggering caspase-mediated apoptotic cell death in HCT116 human colon cancer cells.
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