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首页> 外文期刊>Journal of biological inorganic chemistry: JBIC: a publication of the Society of Biological Inorganic Chemistry >Metals in medicine: metal-related diseases-Cytotoxicity of palladium(II) complexes with 1,10- phenanthroline derivatives and dithiocarbamate as DNA intercalators
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Metals in medicine: metal-related diseases-Cytotoxicity of palladium(II) complexes with 1,10- phenanthroline derivatives and dithiocarbamate as DNA intercalators

机译：医药中的金属：与金属有关的疾病-具有1,10-菲咯啉衍生物和二硫代氨基甲酸酯作为DNA嵌入剂的钯（II）配合物的细胞毒性

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Cisplatin (cis-[PtCl_2(NH_3)_2]; cisPt) has been one of the leading antitumor drug. However, dose-related nephrotoxicity and a variety of toxic side effects are frequently observed with this drug. In addition, some cancers have been reported to obtain resistance by continuously administering cisPt (cisPt-resistant cancers). Therefore, much attention has been focused on the development of new platinum complexes with decrease of the toxic side effects and effectiveness for cisPt-resistant cancers. In this study, Pd(II) complexes with 1,10-phenanthroline derivatives (R-phen) and dimethyldithiocarbamate (dmdt), [Pd(dmdt)(R-phen)]Cl, were synthesized and the interactions of these complexes with CT-DNA investigated using competitive ethidium bromide (EtBr) studies. On adding the complexes to CT-DNA pretreated with EtBr the fluorescence intensity of CT-DNA-bound EtBr decreased. The apparent DNA binding constants (K_(app)) estimated from relevant fluorescence quenching data were Pd-1[Pd-2[Pd-3[Pd-4. Next, the cytotoxic activities of these complexes were determined by MTT assay (IC_(50)). Moreover, the partition coefficients of these complexes (log P_(o/w)) were also obtained by 1-octanol/water system. It is estimated that the difference of IC50 values are attributed to the hydrophobicity (log P_(o/w)). In summary, it is concluded that the cytotoxic activities of these complexes are proportional to the ability of intercalation and hydrophobicity. It is particularly noteworthy that the cytotoxic activity of Pd-2 was 16 times higher than that of cisPt for cisPtsensitive L1210 and 110 times higher than that of cisPt for cisPtresistant L1210.
机译：顺铂（cis- [PtCl_2（NH_3）_2]; cisPt）已成为领先的抗肿瘤药物之一。但是，这种药物经常观察到剂量相关的肾毒性和多种毒性副作用。另外，已经报道了一些癌症通过连续施用顺铂来获得抗药性（顺铂抗性癌症）。因此，许多注意力集中在开发新的铂配合物上，该复合物具有降低的毒副作用和对顺铂耐药的癌症的有效性。在这项研究中，Pd（II）配合物与1,10-菲咯啉衍生物（R-phen）和二甲基二硫代氨基甲酸酯（dmdt）[Pd（dmdt）（R-phen）] Cl合成，并且这些配合物与CT的相互作用-DNA使用竞争性溴化乙锭（EtBr）研究进行了研究。将复合物添加到用EtBr预处理的CT-DNA上，与CT-DNA结合的EtBr的荧光强度降低。从相关的荧光猝灭数据估计的表观DNA结合常数（K_（app））为Pd-1 [Pd-2 [Pd-3 [Pd-4]。接下来，通过MTT测定法（IC_（50））确定这些复合物的细胞毒性活性。此外，这些配合物的分配系数（log P_（o / w））也通过1-辛醇/水系统获得。据估计，IC 50值的差异归因于疏水性（log P_（o / w））。总之，可以得出结论，这些复合物的细胞毒活性与嵌入和疏水性的能力成正比。特别值得注意的是，Pd-2对顺铂敏感的L1210的细胞毒性活性比顺铂高16倍，对顺铂抗性L1210的细胞毒性比顺铂高110倍。

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