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首页> 外文期刊>Life sciences >Growth, morphological and biochemical changes in oxa-spermine derivative-treated MCF-7 human breast cancer cells.
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Growth, morphological and biochemical changes in oxa-spermine derivative-treated MCF-7 human breast cancer cells.

机译：氧精胺衍生物处理的MCF-7人乳腺癌细胞的生长，形态和生化变化。

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摘要

The growth inhibitory properties of two oxa-spermine derivatives named compound 1 and compound 2, representatives of a novel type of polyamine derivatives, were studied. Dose-response growth inhibitory curves obtained after 48h drug exposure demonstrated the much higher cytotoxic activity of compound 1 towards MCF-7 human breast cancer cells. Further experiments with compound 1 showed that this oxa-spermine derivative exhibited considerable cytotoxicity with IC(50) values of 3.74 microM and 2.93 microM after 24h and 48h drug exposure respectively. In MCF-7 cells, after 8h drug (10 microM) exposure it caused shrinkage, chromatin condensation and nuclear fragmentation. However, no clear DNA laddering was detected in treated cells. Drug treatment provoked an increase in polyamine oxidase (PAO) activity. This enzyme is able to produce cytotoxic H(2)O(2) and 3-acetamidopropanal, catalyzing the oxidative deamination of N(1)-acetylated derivatives of spermine and spermidine to spermidine and putrescine respectively. Taken together these data demonstrate that the novel oxa-polyamine derivative compound 1 has considerable cytotoxic activity towards MCF-7 cells and indicate that an induction of PAO may be involved in its cytotoxic and apoptotic effects.
机译：研究了两种新的多胺衍生物代表的氧杂精胺衍生物的生长抑制特性，分别命名为化合物1和化合物2。药物暴露48h后获得的剂量反应生长抑制曲线表明，化合物1对MCF-7人乳腺癌细胞具有更高的细胞毒活性。化合物1的进一步实验表明，该草精胺衍生物在暴露24h和48h后分别具有3.74 microM和2.93 microM的IC（50）值，具有相当大的细胞毒性。在MCF-7细胞中，暴露8h（10 microM）的药物后会引起皱缩，染色质浓缩和核碎裂。但是，在处理过的细胞中未检测到清晰的DNA梯形图。药物治疗引起了多胺氧化酶（PAO）活性的增加。这种酶能够产生细胞毒性的H（2）O（2）和3-乙酰氨基丙醛，分别催化N（1）-乙酰化的亚精胺和亚精胺衍生物分别被氧化成亚精胺和腐胺。这些数据加在一起表明，新型的氧杂多胺衍生物化合物1对MCF-7细胞具有相当大的细胞毒性活性，并表明PAO的诱导可能与其细胞毒性和凋亡作用有关。

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