Konac Ece, Varol Nuray, Kiliccioglu Ilker, Bilen Cenk Y
Department of Medical Biology and Genetics, Faculty of Medicine, Gazi University, Ankara 06500, Turkey.
Department of Urology, Faculty of Medicine, Hacettepe University, Ankara 06100, Turkey.
Oncol Lett. 2015 Jul;10(1):560-564. doi: 10.3892/ol.2015.3250. Epub 2015 May 20.
The proteasome inhibitor bortezomib is a promising novel agent in bladder cancer therapy; however, inducible cytoprotective mechanisms may limit its potential efficacy. To date, the cellular and molecular effects of proteasome inhibitors on bladder cancer cells have been poorly characterized. Despite the consistent rate of initial responses, cisplatin treatment typically results in the development of chemoresistance, leading to therapeutic failure. Therefore, the present study aimed to characterize the molecular mechanisms underlying the anti-proliferative effects of cisplatin and bortezomib combination therapy on the human T24 bladder cancer cell line, by analyzing the protein expression levels of apoptotic genes. Cytotoxic effects were measured using a water-soluble tetrazolium salt-1 assay, and the apoptosis-associated molecules were examined using western blot analysis and ELISA. It was observed that combined administration of cisplatin and bortezomib induced upregulation of caspase-3, -8 and -9, B-cell lymphoma-2 (Bcl-2)-like 11 and Bcl-2-interacting killer, but downregulated Bcl-2 and Bcl-extra large protein expression levels in T24 cells in a dose-dependent manner. Furthermore, enhanced protein expression of caspase-8 and -9, in line with the significantly increased caspase-3 activation, was detected when the cells were treated with a combination of cisplatin and bortezomib, compared with that of either agent alone. Bortezomib appeared to synergize with cisplatin to promote apoptosis via the extrinsic and intrinsic apoptotic pathways. Taken together, the results of the current study provide the preclinical framework for additional evaluation of the effects of combining bortezomib with other agents to induce apoptosis in bladder cancer cells.
蛋白酶体抑制剂硼替佐米是膀胱癌治疗中一种很有前景的新型药物;然而,可诱导的细胞保护机制可能会限制其潜在疗效。迄今为止,蛋白酶体抑制剂对膀胱癌细胞的细胞和分子作用尚未得到充分表征。尽管初始反应率一致,但顺铂治疗通常会导致化疗耐药的产生,从而导致治疗失败。因此,本研究旨在通过分析凋亡基因的蛋白表达水平,来表征顺铂和硼替佐米联合治疗对人T24膀胱癌细胞系抗增殖作用的分子机制。使用水溶性四氮唑盐-1法测定细胞毒性作用,并通过蛋白质印迹分析和酶联免疫吸附测定法检测凋亡相关分子。结果观察到,顺铂和硼替佐米联合给药可诱导T24细胞中半胱天冬酶-3、-8和-9、B细胞淋巴瘤-2(Bcl-2)样蛋白11和Bcl-2相互作用杀伤蛋白的上调,但以剂量依赖的方式下调Bcl-2和Bcl-2相关X蛋白的表达水平。此外,与单独使用任何一种药物相比,当细胞用顺铂和硼替佐米联合处理时,检测到半胱天冬酶-8和-9的蛋白表达增强,这与半胱天冬酶-3激活的显著增加一致。硼替佐米似乎与顺铂协同作用,通过外源性和内源性凋亡途径促进细胞凋亡。综上所述,本研究结果为进一步评估硼替佐米与其他药物联合诱导膀胱癌细胞凋亡的效果提供了临床前框架。