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一维链[Fe(salen)(L)](n)配合物对人癌细胞系的体外细胞毒性评价。

Evaluation of in vitro cytotoxicity of one-dimensional chain [Fe(salen)(L)](n) complexes against human cancer cell lines.

机构信息

Regional Centre of Advanced Technologies and Materials, Department of Cell Biology and Genetics, Faculty of Science, Palacký University, Šlechtitelů 11, CZ-783 71 Olomouc, Czech Republic.

出版信息

Toxicol In Vitro. 2012 Apr;26(3):480-4. doi: 10.1016/j.tiv.2012.01.006. Epub 2012 Jan 17.

Abstract

The 1d-polymeric iron(III) complexes Fe(salen)(μ-L) (1-6), involving a deprotonated form of the N-donor heterocyclic compounds (L) imidazole (complex 1), 1,2,4-triazole (2), benztriazole (3), 5-methyltetrazole (4), 5-aminotetrazole (5) and 5-phenyltetrazole (6), were studied for their in vitro cytotoxic activity against human cancer cell lines including lung carcinoma (A549), cervix epithelial carcinoma (HeLa), osteosarcoma (HOS), malignant melanoma (G361), breast adenocarcinoma (MCF7), ovarian carcinoma (A2780) and cisplatin-resistant ovarian carcinoma (A2780cis). Cytotoxicity in vitro (IC50=0.39-0.48 μM) was achieved for 2-6 against A2780 (IC50 of cisplatin equals 11.5 μM) as well as for 5 and 6 against all the tested cells, with IC50=2.5-37.7 μM. The Uv-Vis spectroscopic study showed that the complexes are unstable in organic solvents (e.g., dimethyl sulfoxide, dimethylformamide) containing even trace amounts of water (and thus also in the medium, i.e., 0.1% DMF, v/v, used in the MTT assay), where they partially or completely decompose to the mixtures involving, besides Fe(salen)(μ-L) itself, also the starting compounds [{Fe(salen)}2(μ-O)] and appropriate organic compound (HL). In efforts to find how the resulting cytotoxicity of the most active compounds 5 and 6 is influenced by this fact, the in vitro cytotoxicity testing of mixtures of reactants [{Fe(salen)}2(μ-O)] and HL, as well as the respective reactants, was also performed. It has been found that the cytotoxicity of 5 and 6 against all the tested cell lines is probably caused by a combined effect of the individual components presented within the corresponding mixture in the medium used.

摘要

标题

1d-聚合铁(III)配合物[Fe(salen)(μ-L)] (n) (1-6)对人癌细胞系的体外细胞毒性研究

研究了 1d-聚合铁(III)配合物[Fe(salen)(μ-L)] (n) (1-6),其中涉及 N-供体杂环化合物(L)咪唑(配合物 1)、1,2,4-三唑(2)、苯并三唑(3)、5-甲基四唑(4)、5-氨基四唑(5)和 5-苯基四唑(6)的去质子形式。这些配合物对人癌细胞系(包括肺癌(A549)、宫颈上皮癌(HeLa)、骨肉瘤(HOS)、恶性黑色素瘤(G361)、乳腺癌(MCF7)、卵巢癌(A2780)和顺铂耐药卵巢癌(A2780cis))的体外细胞毒性进行了研究。配合物 2-6 对 A2780 的体外细胞毒性(IC50=0.39-0.48 μM)与顺铂的 IC50(IC50 of cisplatin equals 11.5 μM)相当,而配合物 5 和 6 对所有测试的细胞均具有细胞毒性,IC50=2.5-37.7 μM。紫外可见光谱研究表明,配合物在含有痕量水的有机溶剂(如二甲基亚砜、二甲基甲酰胺)中不稳定(因此也在介质中不稳定,即 0.1% DMF,v/v,用于 MTT 测定),在这些溶剂中,它们部分或完全分解为混合物,除了[Fe(salen)(μ-L)] (n)本身外,还包括起始化合物[{Fe(salen)}2(μ-O)]和适当的有机化合物(HL)。为了研究最活跃的化合物 5 和 6 的这种毒性如何受到这一事实的影响,还对反应物[{Fe(salen)}2(μ-O)]和 HL 的混合物以及相应的反应物的体外细胞毒性进行了测试。研究发现,5 和 6 对所有测试细胞系的细胞毒性可能是由于在所用介质中相应混合物中存在的各个成分的综合作用所致。

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