关键词: 槲皮素衍生物, 膀胱癌, 细胞周期

Abstract: 【Abstract】〓Objective〓To investigate the in vitro and in vivo effects of quercetin and its derivative (quercetin-7-sulphate) on human bladder cancer cells by using the BIU-87 cell line and nude mice. Methods〓The BIU-87 cells were exposed to different concentrations of quercetin and sodium quercetin-7-sulphate (SQMS). Cell proliferation and the half maximal inhibitory concentration (IC50) values were determined by MTT assay, and cell cycle was evaluated by flow cytometry. Tumor masses were weighed and tumor inhibition rate were calculated in tumor bearing mice treated with quercetin and SQMS at low, medium and high concentration respectively. Tumor tissue specimen were processed for histological analysis. The expression levels of Ki-67, Cyclin D1 and Cyclin B1 were evaluated by using immunohistochemistry..Results〓Both quercetin and SQMS showed inhibitory effects on proliferation in BIU-87 cells in a dose-dependent manner,.with no statistically significant difference observed between quercetin and SQMS groups of the same concentration.(P>0.05). Quecertin significantly arrested the growth of BIU-87 cells at G2/M phase,.while SQMS mainly arrested them at G0/G1 phase..The in vivo tumor inhibition capacity of quecertin was comparable to that of SQMS administrated at medium concentration(P>0.05)..Quecertin more potently down-regulated the expression of Cyclin B1.(P<0.05).while SQMS more potently down-regulated the expression of CyclinD1 (P<0.01). But there was no significant effect on Ki-67 expression (P>0.05). Conclusion〓Both quercetin and SQMS showed a significant anti-tumor effect not only on the BIU-87 bladder cancer cell line but also on bladder carcinoma in nude mice. Medium concentration SQMS showed similar in vivo inhibitory effect to that of quercetin. Quecertin significantly arrested bladder cancer cells at G2/M phase probably by down-regulating the expression of Cyclin B1,.while SQMS significantly arrested the cancer cells at G0/G1 phase,.at least partly,.by down-regulating the expression of CyclinD1.

Key words: Quercetin, Derivatives bladder carcinoma, Cell cycle