| 3,4-dihydroxycinnamic acid (caffeic acid) is a natural compound containing cinnamic acid structure, abounding in coffee, fruits, vegetables and grains. It is reported that 3,4-dihydroxycinnamic acid is a potent chemopreventive agent. However, the antitumor effects of 3,4-dihydroxycinnamic acid in vivo and in vitro have not been reported. Due to the poor solubility of 3,4-dihydroxycinnamic acid in water, we transformed it to its sodium salt. In the first three parts of this paper, the antitumor biochemical modulation of sodium 3,4-dihydroxycinnamate (DCA-Na) is reported.Tea is one of the most common beverages consumed worldwide. Many epidemiological studies suggest that green tea consumption can prevent cancer. Our previous work have found that green tea extract enhances the cytotoxic effect of AraC and MTX. In the fourth part of this paper, the antitumor biochemical modulation of epigallocatechin-3-gallate (EGCG), which is a main constituent in green tea extract, is reported.1. Antitumor effects of sodium 3,4-dihydroxycinnamateNucleoside transport assay proved that DCA-Na inhibited moderately the nucleoside transport in human hepatoma BEL-7402 cells with an IC50 about 1000 μg/ml. DCA-Na inhibited the proliferation of huamn leukemia HL-60 cells, human squamous carcinoma KB cells and hepatoma BEL-7402 cells, with IC50 values ranging from 100 to 200 μg/ml as determined by MTT assay. DCA-Na inhibited the clonogenecity of KB cells and BEL-7402 cells with IC50 values from 0.5 to 3 μg/ml. The effects of DCA-Na were time-dependent and dose-dependent.Experiments in vivo indicated that DCA-Na inhibited the growth of transplanted tumors including hepatoma 22 and colon carcinoma 26 in mice. The inhibition rates ranged between 41% and 55% at the dose of 1 g/kg. No obvious toxicity occurred in the mice. Moreover, DCA-Na inhibited the metastasis of transplanted Lewis lung carcinoma in mice with an inhibition of 55% at the dose of 1 g/kg. |
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