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Cytotoxicity of gold(III) complexes on A549 human lung carcinoma epithelial cell line

机译:金(III)配合物对A549人肺癌上皮细胞系的细胞毒性

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We have studied the kinetics of the complex formation of gold(III) complexes, [Au(en)Cl 2] + (dichlorido(ethylendiamine) aurate(III)-ion) [Au(dach)Cl 2] (dichloride(1,2-diaminocyclohexane) aurate(III)-ion) and [Au(bipy)Cl 2] + (dichlorido(2, 2′-bipyridyl)aurate(III)-ion) with guanosine5′-monophosphate (5′-GMP). It was shown that 5′-GMP have a high affinity for gold(III) complex, which may have important biological implications, since the interactions of Au(III) with DNA are thought to be responsible for the anti-tumor activity. The [Au(bipy)Cl 2] + complex is more reactive than [Au(en)Cl 2] + or [Au(dach)Cl 2] +. The activation parameters for all studied reactions suggest an associative substitution mechanism. The cytotoxicity of gold(III) complexes was tested on A549 human lung carcinoma epithelial cell line and was evaluated by cytotoxic (MTT and LDH test) and apoptotic assays. The results showed that all tested gold(III) complexes displayed cytotoxic effect on A549 cells. Among the tested gold (III) complexes, AuBIPY showed the best cytotoxic effects.
机译:我们研究了金(III)络合物[Au(en)Cl 2] +(二氯基(乙基乙二胺)金(III)-离子)[Au(dach)Cl 2](二氯化物(1,带有鸟苷5'-单磷酸酯(5'-GMP)的2-二氨基环己烷)金酸酯(III)-离子和[Au(bipy)Cl 2] +(二氯基(2,2'-联吡啶基)金酸酯(III)-离子)。结果表明5'-GMP对金(III)配合物具有很高的亲和力,这可能具有重要的生物学意义,因为据认为Au(III)与DNA的相互作用是抗肿瘤活性的原因。 [Au(bipy)Cl 2] +络合物比[Au(en)Cl 2] +或[Au(dach)Cl 2] +具有更高的反应性。所有研究的反应的激活参数都暗示了一种关联取代机制。在A549人肺癌上皮细胞系上测试了金(III)配合物的细胞毒性,并通过细胞毒性(MTT和LDH测试)和凋亡分析进行了评估。结果表明,所有测试的金(III)配合物均显示出对A549细胞的细胞毒性作用。在测试的金(III)配合物中,AuBIPY显示出最佳的细胞毒性作用。

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