Huang X X, Wang R X, Lin Q, Chen W, Pan Y, Wang S Q, Weng Z L, Huang W P
Pharmazie. 2017 Feb 1;72(2):87-90. doi: 10.1691/ph.2017.6839.
Recently, 2-methoxyestradiol (2-ME) has been considered to be a potential anticancer agent but has not been investigated in bladder cancer. This study was conducted to clarify the role of 2-ME in bladder cancer cells. The bladder cancer cell line T-24 was treated with 2 μm 2-ME for 2 d. The T-24 cell viability, colony formation, invasion and apoptosis were observed in 2-ME-treated and control cells. The expression of hypoxia-inducible factor 1 alpha (HIF-1α) was detected using reverse transcription-polymerase chain reaction (RT-PCR). Then western blotting assay was applied to assess expressions of HIF-1α and apoptosis factors caspase-3 and Bcl-x proteins. The mRNA and protein expressions of HIF-1α in 2-ME-treated T-24 cells were remarkably lower than that of the control cells (P < 0.05). Treatment of 2-ME could significantly inhibit T-24 the cell viability, colony formation, invasion, and promote apoptosis (all P < 0.05). In addition, the protein expression of Caspase-3 was higher and that of Bcl-x protein was lower after administration of 2-ME compared to control (both P < 0.05). Collectively, we characterized the efficacy of 2-ME on bladder cancer T-24 cells as being mediated by inhibition of cell viability, colony fomation, invasion and promoting cell apoptosis, which may be achieved by suppressing HIF-1α levels. This study suggests 2-ME as a potential drug for bladder cancer therapy.
最近，2-甲氧基雌二醇（2-ME）被认为是一种潜在的抗癌药物，但尚未在膀胱癌中进行研究。本研究旨在阐明2-ME在膀胱癌细胞中的作用。将膀胱癌细胞系T-24用2 μM 2-ME处理2天。观察2-ME处理组和对照组细胞的T-24细胞活力、集落形成、侵袭和凋亡情况。采用逆转录-聚合酶链反应（RT-PCR）检测缺氧诱导因子1α（HIF-1α）的表达。然后应用蛋白质印迹分析评估HIF-1α以及凋亡因子半胱天冬酶-3和Bcl-x蛋白的表达。2-ME处理的T-24细胞中HIF-1α的mRNA和蛋白表达明显低于对照组细胞（P < 0.05）。2-ME处理可显著抑制T-24细胞活力、集落形成、侵袭，并促进细胞凋亡（均P < 0.05）。此外，与对照组相比，给予2-ME后半胱天冬酶-3的蛋白表达升高，Bcl-x蛋白的表达降低（均P < 0.05）。总体而言，我们发现2-ME对膀胱癌细胞T-24的作用是通过抑制细胞活力、集落形成、侵袭以及促进细胞凋亡来介导的，这可能是通过抑制HIF-1α水平实现的。本研究表明2-ME是一种潜在的膀胱癌治疗药物。
