Synthesis, characterization, and cytotoxic properties of mono- and di-nuclear cobalt(ii)-polypyridyl complexes†‡,Dalton Transactions

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Synthesis, characterization, and cytotoxic properties of mono- and di-nuclear cobalt(ii)-polypyridyl complexes†‡
Dalton Transactions ( IF 3.5 ) Pub Date : 2018-03-16 00:00:00 , DOI: 10.1039/c8dt00577j
Arvin Eskandari _{1,

2,

3,

4} , Arunangshu Kundu _{1,

5,

6,

7} , Chunxin Lu _{8,

9,

10,

11} , Sushobhan Ghosh _{1,

5,

6,

7} , Kogularamanan Suntharalingam _{1,

2,

3,

4}

Affiliation

We report the synthesis and characterisation of mono- and di-nuclear cobalt(II) complexes (1–3) containing L¹, a polypyridyl ligand with pyrazole moieties. DNA binding studies suggest that the mono-nuclear complex, 1, binds to DNA via the grooves prior to inducing oxidative DNA cleavage whereas the larger di-nuclear complexes, 2 and 3, bind to DNA via the grooves and through intercalation prior to inducing oxidative DNA cleavage. The cobalt(II) complexes display micromolar potency towards U2OS (bone osteosarcoma), HepG2 (liver hepatocellular carcinoma), and GM05757 (normal human fibroblast) cells, comparable to clinically used platinum agents, cisplatin and carboplatin. The cellular mechanism of action studies show that the most effective cobalt(II) complex, 2, enters U2OS cells, penetrates the nucleus, induces genomic DNA damage, and triggers caspase-dependent apoptosis in a p53-independent manner. This study highlights the potential of di-nuclear cobalt(II) complexes as artificial oxidative metallonucleases and tangible cancer cell-potent agents.

中文翻译：

合成，表征，和单-和二-核钴的细胞毒性特性（II）配合物-polypyridyl †往最 ‡

我们报告了单核和双核钴（II）配合物（1-3）的合成和表征，其中配合物L ¹为带有吡唑基团的多吡啶基配体。DNA结合研究表明，单核复合物1在诱导氧化性DNA裂解之前通过凹槽与DNA结合，而较大的双核复合物2和3在诱导氧化性裂解之前通过凹槽并通过嵌入与DNA结合。DNA切割。钴（二）复合物对U2OS（骨骨肉瘤），HepG2（肝肝细胞癌）和GM05757（正常人成纤维细胞）细胞具有微摩尔效价，与临床使用的铂试剂，顺铂和卡铂相当。细胞作用机制研究表明，最有效的钴（II）复合物2进入U2OS细胞，穿透细胞核，诱导基因组DNA损伤，并以p53独立的方式触发caspase依赖性凋亡。这项研究强调了双核钴（II）复合物作为人工氧化金属核酸酶和有形癌细胞活性剂的潜力。

更新日期：2018-03-16

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