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Abstract: Kaempferol-7-O-β-d-glucoside (KG), a flavonoid glycoside, isolated from Smilax china L. rhizome, displayed marked anticancer activity on a panel of established cancer cells, of which, HeLa human cervix carcinoma cells were the most sensitive. Meanwhile, the cytotoxic effects of KG on normal human cells (HEK293 embryonic kidney cells and L-02 embryonic liver cells) were much smaller than on cancer cells. This work studied the molecular mechanisms underlying KG induced growth inhibition in HeLa cells. The results showed that KG induced G2/M phase growth arrest correlated with Cyclin B1 and Cdk1 decrease in a p53-independent manner, and also caused an increase in apoptosis, which was confirmed by characteristic morphological changes, evident DNA fragmentation, increased apoptotic sub-G1 population. Furthermore, inhibition of NF-κB nuclear translocation, up-regulation of Bax and down-regulation of Bcl-2, were observed in HeLa cells treated with KG, which indicated that the mitochondrial pathway was involved in the apoptosis signal pathway. In summary, KG displayed a significant anti-tumor effect through cell cycle arrest and apoptotic induction in HeLa cells, which suggested that KG might have therapeutic potential against cervix carcinoma. [Copyright &y& Elsevier]

A human carcinoma xenograft model was established with resistant KB-A-1 cell line in order to investigate whether (-)-epigallocatechin gallte (EGCG) can reverse doxorubicin (DOX) resistance in vivo. EGCG could sensitize the tumors to DOX as indicated by a considerable reduction of tumor weights. The combination of DOX with EGCG increased the DOX concentration by 51% in the tumors, and increased DOX-induced apoptosis in the tumors compared with DOX alone. In addition, the combination schedules appeared to be well tolerated. We conclude that EGCG could chemosensitize resistant tumor cells to DOX in vivo through an increase in the accumulation of DOX in the tumors. [Copyright &y& Elsevier]