首页> 外文期刊>Bioorganic and medicinal chemistry >Synthesis, structural characterization and cell death-inducing effect of novel palladium(II) and platinum(II) saccharinate complexes with 2-(hydroxymethyl)pyridine and 2-(2-hydroxyethyl)pyridine on cancer cells in vitro
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Synthesis, structural characterization and cell death-inducing effect of novel palladium(II) and platinum(II) saccharinate complexes with 2-(hydroxymethyl)pyridine and 2-(2-hydroxyethyl)pyridine on cancer cells in vitro

机译:新型2-(羟甲基)吡啶和2-(2-羟乙基)吡啶糖精钯(II)和糖精铂(II)配合物的合成,结构表征和细胞死亡诱导作用

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摘要

Four palladium(II) and platinum(II) saccharinate (sac) complexes with 2-(hydroxymethyl)pyridine (2-hmpy) and 2-(2-hydroxyethyl)pyridine (2-hepy), namely trans-[Pd(2-hmpy)2(sac)2]·H2O (1), trans-[Pt(2-hmpy)2(sac)2]·3H2O (2), trans-[Pd(2-hepy)2(sac)2] (3) and trans-[Pt(2-hepy) 2(sac)2] (4), have been synthesized and characterized by elemental analysis, UV-vis, IR and NMR. Single crystal X-ray analysis reveals that the metal(II) ions in each complex are coordinated by two sac and two 2-hmpy or 2-hepy ligands with a trans arrangement. Anticancer effects of 1-4 were tested against four different cancer cell lines (A549 and PC3 for lung cancer, C6 for glioblastoma, and Hep3B for liver cancer). Cytotoxicity was first screened by the MTT assay and the results were further confirmed by the ATP assay. The mode of cell death was determined by both histological and biochemical methods. Among the metal complexes, complex 2 resulted in relatively stronger anti-growth effect in a dose-dependent manner (3.13-200 μM), compared to the others, by inducing apoptosis.
机译:四种具有2-(羟甲基)吡啶(2-hmpy)和2-(2-羟乙基)吡啶(2-hepy)的糖精钯(II)和糖精(sac)配合物,即反式[Pd(2- hmpy)2(sac)2]·H2O(1),反式[Pt(2-hmpy)2(sac)2]·3H2O(2),反式-[Pd(2-hepy)2(sac)2] (3)和反式-[Pt(2-hepy)2(sac)2](4)已合成并通过元素分析,UV-vis,IR和NMR进行了表征。单晶X射线分析表明,每个络合物中的金属离子均由两个囊和两个带有反式排列的2-hmpy或2-hepy配体配位。测试了1-4种抗癌作用对四种不同癌细胞系的影响(针对肺癌的A549和PC3,针对成胶质细胞瘤的C6和针对肝癌的Hep3B)。首先通过MTT试验筛选细胞毒性,然后通过ATP试验进一步证实结果。细胞死亡的方式通过组织学和生化方法确定。在金属配合物中,与其他配合物相比,配合物2通过诱导细胞凋亡以剂量依赖性方式(3.13-200μM)产生了相对较强的抗生长作用。

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