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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Potential cytotoxic and amoebicide activity of first row transition metal compounds with 2,9-bis-(2′,5′-diazahexanyl)-1,1-phenanthroline (L1)
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Potential cytotoxic and amoebicide activity of first row transition metal compounds with 2,9-bis-(2′,5′-diazahexanyl)-1,1-phenanthroline (L1)

机译：具有2,9-双-（2'，5'-二氮杂己基）-1,1-菲咯啉（L1）的第一排过渡金属化合物的潜在细胞毒性和杀螨活性

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摘要

A new synthetic pathway was reported to obtain N6 donor ligand 2,9-bis-(2′,5′-diazahexanyl)-1,10-phenanthroline (L1) and its coordination compounds of essential divalent metal ions Mn, Fe, Co, Ni, Cu and Zn. Complete characterization of all compounds was done with the conventional techniques. Crystal structures of [NiL1](PF _6) _2 and [ZnL1](PF _6) _2·H _2O were also reported. Electrochemical studies have shown an active participation of the aromatic moiety of the ligand in redox reactions. The in vitro tests of the cytotoxic activity against human tumour cell lines HeLa (cervix) and CHP-212 (neuroblastoma) showed that all coordination compounds that involve redox active metal ions exhibit noteworthy antiproliferative activity, superior in all cases to cisplatin. [CuL1] ~(2+) showed the lower IC _(50) value in the HeLa cell line with 1.84 μM, meanwhile, [CoL1] ~(2+) showed the lower value in neuroblastoma CHP-212 with IC _(50) = 45.28 μM. None of these compounds were active against the SK-N-SH neuroblastoma cell line. In Entamoeba histolytica cultures, remarkable nanomolar IC _(50) values were found for [NiL1] ~(2+) and [MnL1] ~(2+) with 60 nM and 80 nM respectively, improving the antiproliferative activity more than 1000 times compared with the first choice drug for clinical treatments of human amoebiasis, metronidazole. On the other hand, a free ligand does not show antiproliferative activity either on human tumor cell lines or on Entamoeba histolytica trophozoites, highlighting the role played by metal ions to produce cytotoxicity in tumor cells and protozoa systems.
机译：据报道，一条新的合成途径获得了N6供体配体2,9-双-（2'，5'-二氮杂己基）-1,10-菲咯啉（L1）及其必需二价金属离子Mn，Fe，Co的配位化合物，镍，铜和锌。所有化合物的完整表征均通过常规技术完成。还报道了[NiL1]（PF _6）_2和[ZnL1]（PF _6）_2·H _2O的晶体结构。电化学研究表明，配体的芳族部分积极参与氧化还原反应。体外测试对人肿瘤细胞HeLa（宫颈）和CHP-212（神经母细胞瘤）的细胞毒性活性表明，所有涉及氧化还原活性金属离子的配位化合物均具有显着的抗增殖活性，在所有情况下均优于顺铂。 [CuL1]〜（2+）在HeLa细胞系中的IC _（50）值较低，为1.84μM，而[CoL1]〜（2+）在成神经细胞瘤CHP-212中的IC _（50）值较低。 ）= 45.28μM。这些化合物都没有针对SK-N-SH神经母细胞瘤细胞系的活性。在组织变形虫培养物中，发现[NiL1]〜（2+）和[MnL1]〜（2+）的纳摩尔IC _（50）值分别为60 nM和80 nM，提高了1000倍以上的抗增殖活性甲硝唑是用于治疗人阿米巴病的首选药物。另一方面，游离配体在人肿瘤细胞系或组织解脂变形杆菌属滋养体上均未显示抗增殖活性，突出了金属离子在肿瘤细胞和原生动物系统中产生细胞毒性的作用。

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