Ilex kudingcha C.J. Tseng (Kudingcha) is a traditional Chinese drink consumed in East Asia. The present study evaluated the in vitro anticancer effects of Kudingcha in MCF-7 human breast adenocarcinoma cells using a 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide (MTT) assay. At a concentration of 200 μg/ml, Kudingcha inhibited the growth of the MCF-7 cells by 81%. This was a greater degree of inhibition than that observed at concentrations of 100 and 50 μg/ml (58 and 19%, respectively). To elucidate the inhibitory mechanisms underlying the anticancer effect of Kudingcha in cancer cells, the expression of genes associated with apoptosis and inflammation were measured using RT-PCR. Kudingcha significantly induced apoptosis, as determined by 4,6-diamidino-2-phenylindole (DAPI) staining, by upregulating Bax, caspase-3 and caspase-9, and downregulating Bcl-2. The expression of the NF-κB, iNOS and COX-2 genes associated with inflammation was significantly decreased (P<0.05) by Kudingcha, thus demonstrating its anti-inflammatory properties. Kudingcha has been reported to exhibit inhibitory effects of tumor metastasis induced in 26-M3.1 colon carcinoma cells in BALB/c mice. The results demonstrated that Kudingcha had potent in vitro anticancer effects; it induced apoptosis, had anti-inflammatory activities and exerted in vivo anti-metastatic effects. Additionally, the anticancer, anti-inflammatory and anti-metastatic effects of Kudingcha were stronger at high concentrations than at low concentrations.