两种新型合成药物对人乳腺癌MCF-7细胞的选择性细胞毒性活性。
Selective cytotoxic activities of two novel synthetic drugs on human breast carcinoma MCF-7 cells.
作者信息
Badisa Ramesh B, Darling-Reed Selina F, Joseph Patrick, Cooperwood John S, Latinwo Lekan M, Goodman Carl B
机构信息
College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL-32307, USA.
出版信息
Anticancer Res. 2009 Aug;29(8):2993-6.
BACKGROUND
Breast cancer is the second leading cause of cancer deaths in US women. We evaluated two novel compounds, piperidinyl-diethylstilbestrol (DES) and pyrrolidinyl-diethylstilbestrol (DES) for cytotoxicity against brine shrimp larvae, MCF-7 and rat normal liver cells.
MATERIALS AND METHODS
In vivo cytotoxicity was evaluated against shrimp larvae for 24 h, while in vitro cell toxicity was evaluated by dye binding crystal-violet method after 48 h. The role of these compounds on different phases of the cell cycle was assessed by flow cytometry.
RESULTS
In shrimp assay, piperidinyl-DES and pyrrolidinyl-DES were potent with 50% effective dose (ED(50)) values of 7.9+/-0.38 and 15.6+/-1.3 microM, respectively. In MCF-7 and normal liver cells, the 50% lethal concentration (LC(50)) values were 19.7+/-0.95, 17.6+/-0.4 microM and 35.1 and >50 microM, respectively. Cell cycle analyses indicated that MCF-7 cells were arrested at the G(0)/G(1) stage with these compounds.
CONCLUSION
The results indicate that pyrrolidinyl-DES possesses highly selective, potent anticancer activity.
背景
乳腺癌是美国女性癌症死亡的第二大主要原因。我们评估了两种新型化合物，哌啶基二乙己烯雌酚（DES）和吡咯烷基二乙己烯雌酚（DES）对卤虫幼虫、MCF-7细胞和大鼠正常肝细胞的细胞毒性。
材料与方法
评估对虾幼虫24小时的体内细胞毒性，而48小时后通过染料结合结晶紫法评估体外细胞毒性。通过流式细胞术评估这些化合物在细胞周期不同阶段的作用。
结果
在对虾试验中，哌啶基-DES和吡咯烷基-DES具有强效，50%有效剂量（ED(50)）值分别为7.9±0.38和15.6±1.3微摩尔。在MCF-7细胞和正常肝细胞中，50%致死浓度（LC(50)）值分别为19.7±0.95、17.6±0.4微摩尔以及35.1和>50微摩尔。细胞周期分析表明，MCF-7细胞与这些化合物一起停滞在G(0)/G(1)期。
结论
结果表明吡咯烷基-DES具有高度选择性的强效抗癌活性。
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