Faculty of Medicine, University of Kragujevac, Kragujevac, Serbia.
Med Chem. 2012 Jan;8(1):2-8. doi: 10.2174/157340612799278469.
We have studied the kinetics of the complex formation of gold(III) complexes, [Au(en)Cl2]+ (dichlorido( ethylendiamine)aurate(III)-ion) [Au(dach)Cl2] (dichloride(1,2-diaminocyclohexane)aurate(III)-ion) and [Au(bipy)Cl2]+ (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)Cl2]+ complex is more reactive than [Au(en)Cl2]+ or [Au(dach)Cl2]+. 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.
我们研究了金(III)配合物与鸟苷 5'-单磷酸（5'-GMP）形成配合物的动力学。实验表明，5'-GMP 与金(III)配合物具有高亲和力，这可能具有重要的生物学意义，因为 Au(III)与 DNA 的相互作用被认为是抗肿瘤活性的原因。[Au(bipy)Cl2]+配合物比[Au(en)Cl2]+或[Au(dach)Cl2]+更具反应性。所有研究反应的活化参数表明存在缔合取代机制。通过细胞毒性（MTT 和 LDH 试验）和凋亡试验测试了金(III)配合物对 A549 人肺腺癌细胞系的细胞毒性，并进行了评估。结果表明，所有测试的金(III)配合物对 A549 细胞均显示出细胞毒性作用。在测试的金(III)配合物中，AuBIPY 表现出最好的细胞毒性作用。
