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Dimethyladamantylmaleimide-induced in vitro and in vivo growth inhibition of human colon cancer Colo205 cells.

机译:二甲基金刚烷基马来酰亚胺诱导的人结肠癌Colo205细胞的体外和体内生长抑制。

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The effect of N-1-(3,5-dimethyladamantyl)maleimide (DMAMI) on the growth of Colo205 human colon cancer cells was examined both in vitro and in vivo. Flow cytometry analysis showed a decrease of G2/M Colo205 cells at 4-6 h after treatment with DMAMI prior to accumulation of apoptotic cells at 24 h. Significant changes in cell morphology, i.e. shrinkage and chromatin condensation of cells, were observed after treatment with DMAMI. In the analysis of the apoptosis markers, it was found that the increase of Annexin V binding to membrane, peroxide radicals, dissipation of the mitochondrial membrane potential, and the activation of caspase-3, -8 and -9 were all evident at 4-6 h after treatment with DMAMI. In vivo analysis showed that treatment of Colo205 tumor-bearing SCID mice with DMAMI (230 mg/kg, intratumoral, once) resulted in rapid tumor damage that leads to significant tumor growth inhibition and no obvious acute toxicity. These results suggest that DMAMI has potential for local treatment of cancer.
机译:在体外和体内均检测了N-1-(3,5-二甲基金刚烷基)马来酰亚胺(DMAMI)对Colo205人结肠癌细胞生长的影响。流式细胞仪分析显示在用DMAMI处理后4-6小时,G2 / M Colo205细胞减少,而在24小时凋亡细胞蓄积。用DMAMI处理后,观察到细胞形态发生了显着变化,即细胞收缩和染色质浓缩。在细胞凋亡标记的分析中,发现膜上膜联蛋白V的结合,过氧化物自由基,线粒体膜电位的耗散以及caspase-3,-8和-9的活化均在4-时明显。用DMAMI处理后6小时。体内分析表明,用DMAMI(230 mg / kg,瘤内,一次)治疗Colo205荷瘤SCID小鼠会导致快速的肿瘤损伤,从而导致明显的肿瘤生长抑制并且没有明显的急性毒性。这些结果表明,DMAMI具有用于癌症局部治疗的潜力。

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