Platinum(II)/palladium(II) complexes with n-propyldithiocarbamate and 2,2′-bipyridine: synthesis, characterization, biological activity and interaction with calf thymus DNA

H. Mansouri‐Torshizi, S. Shahraki, Z. Nezami, A. Ghahghaei, Sahebeh Najmedini, A. Divsalar, Hamed Ghaemi, A. Saboury
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引用次数: 26

Abstract

Two Pd(II) and Pt(II) complexes ([Pt(bpy)(pr-dtc)]Br and [Pd(bpy)(pr-dtc)]Br, where bpy=2, 2′-bipyridine and pr-dtc = n-propyldithiocarbamate) were synthesized and characterized by elemental analysis (CHN), molar conductivity measurements, Fourier transform infrared, 1H nuclear magnetic resonance and UV–visible techniques. In these complexes, the dithiocarbamato ligand coordinates to Pt(II) or Pd(II) center as bidentate with two sulfur atoms. The binding of these complexes to calf thymus DNA (CT-DNA) was investigated using various physicochemical methods such as spectrophotometric, spectrofluorometric and gel filtration technique. The experimental results indicate that Pt(II) and Pd(II) complexes interact with CT-DNA in the intercalative mode. Both complexes unexpectedly denatured DNA at low concentration. Gel filtration studies indicated that the binding of complexes with DNA is strong enough and does not break readily. The cytotoxic activity of these metal complexes has been tested against human cell tumor lines (K562) and revealed much lower 50% cytotoxic concentration (Cc50) less than that of cisplatin. Several binding and thermodynamic parameters are also described.
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铂(II)/钯(II)配合物与n-丙基二硫氨基甲酸酯和2,2 ' -联吡啶:合成、表征、生物活性及其与小牛胸腺DNA的相互作用
合成了两个Pd(II)和Pt(II)配合物[Pt(bpy)(pr-dtc)]Br和[Pd(bpy)(pr-dtc)]Br,其中bpy= 2,2 ' -联吡啶和pr-dtc = n-丙基二硫代氨基甲酸酯),并通过元素分析(CHN)、摩尔电导率测量、傅里叶变换红外、1H核磁共振和紫外可见技术对其进行了表征。在这些配合物中,二硫脲配体与Pt(II)或Pd(II)中心呈双齿状配位,具有两个硫原子。利用分光光度法、荧光光谱法和凝胶过滤技术等多种理化方法研究了这些复合物与小牛胸腺DNA (CT-DNA)的结合。实验结果表明,Pt(II)和Pd(II)配合物以插层方式与CT-DNA相互作用。这两种复合物在低浓度下出人意料地使DNA变性。凝胶过滤研究表明,复合物与DNA的结合足够强,不易断裂。这些金属配合物的细胞毒活性对人肿瘤细胞系(K562)进行了测试,显示其细胞毒浓度(Cc50)远低于顺铂的50%。还描述了几个结合和热力学参数。
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