Purpose: It has been shown that some of ginger derivatives possess antitumor activity (such as [6]-gingerol and [6]-paradol), but the antitumor activity of other skeletal derivatives have not yet been determined. We have synthesized new gingerdione derivatives and found that they could inhibit human leukemia cells growth. The purpose of this study is to determine the action mechanism of gingerdione derivatives on human leukemia cells. Methods: Human leukemia cells were treated with newly synthesized gingerdione derivatives or vehicles. Cellular proliferation rate was determined by MTT assay. Antitumor mechanisms were determined by using cell cycle analysis, DNA fragmentation, and RT-PCR technology. Results: Among the newly synthesized compounds, we found that 1-(3, 4-dimethoxyphenyl)-3, 5-tetradecenedione (I8) is most effective against HL-60 cells with IC50 values of approximately 22.4μM. Furthermore, I8 may exert its antitumor action by inducing cell cycle arrest at G0/G1 phase and promoting cell apoptosis. Conclusions: Among the newly synthesized compounds, we found that I8 is most effective against leukemia cells. Therefore, I8 may have potential to be developed as a novel antitumor agent.
