Synthesis and biological evaluation of quercetin-zinc (II) complex for anti-cancer and anti-metastasis of human bladder cancer cells

摘要

Bladder cancer is the 13th leading cause of cancer death worldwide, and its mortality rate is highly associated with the motility of the malignant cells. Although the techniques of urothelial cancer treatment have been continuously advanced in the last decade, the invasive bladder cancer remains incurable and the mean survival time of the patients with high-grade malignancy after cancer relapse is still <6months, indicating a new strategy which can reduce bladder cancer cell motility and/or progression is urgently needed. Quercetin is a polyphenolic flavonoid with approved anti-tumor effect. However, the drawbacks of quercetin, including low absorption, extensive metabolism, and rapid elimination, severely hamper its availability in the clinic. In this study, we aim to synthesize the quercetin-zinc complex (Q-ZnCPX) and explore its anti-cancer and anti-metastasis efficacies on human bladder cancer cells in vitro. Based on the results of cell movement and protein expressions in BFTC-905 cells, we found that both cell migratability and invasiveness were markedly reduced by the Q-ZnCPX with concentration of 12.5M through p-AKT and MT1-MMP regulations compared to the cells without treatment (P<0.05). Moreover, the synthesized Q-ZnCPX with 75M can even provide >50% of mortality rate (P<0.05) to the cancer cell after 24-h treatment. These results demonstrated that the synthetic Q-ZnCPX may serve as feasible tool for both anti-cancer and anti-metastasis on human bladder cancer cells dependent on the dosage.