Departamento de Química Inorgánica, Facultade de Química, Campus Vida, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
Departamento de Bioquímica y Biología Molecular, Facultade de Veterinaria, Campus Terra, Universidade de Santiago de Compostela, 27002 Lugo, Spain.
Int J Mol Sci. 2023 Jan 23;24(3):2246. doi: 10.3390/ijms24032246.
The design of artificial helicoidal molecules derived from metal ions with biological properties is one of the objectives within metallosupramolecular chemistry. Herein, we report three zinc helicates derived from a family of thiosemicarbazone ligands with different terminal groups, Zn(L)∙2HO , Zn(L)∙2HO and Zn(L), obtained by an electrochemical methodology. These helicates have been fully characterized by different techniques, including X-ray diffraction. Biological studies of the zinc(II) helicates such as toxicity assays with erythrocytes and interaction studies with proteins and oligonucleotides were performed, demonstrating in all cases low toxicity and an absence of covalent interaction with the proteins and oligonucleotides. The in vitro cytotoxicity of the helicates was tested against MCF-7 (human breast carcinoma), A2780 (human ovarian carcinoma cells), NCI-H460 (human lung carcinoma cells) and MRC-5 (normal human lung fibroblasts), comparing the IC values with cisplatin. We will try to demonstrate if the terminal substituent of the ligand precursor exerts any effect in toxicity or in the antitumor activity of the zinc helicates.
设计具有生物特性的金属离子衍生的人工螺旋分子是金属超分子化学的目标之一。在此，我们报告了三种锌螺旋配合物，它们是由一系列具有不同末端基团的硫代半卡巴腙配体衍生而来的，通过电化学方法得到 Zn(L)∙2HO 、Zn(L)∙2HO 和 Zn(L)。这些螺旋配合物已经通过多种技术进行了全面表征，包括 X 射线衍射。对锌（II）螺旋配合物进行了生物学研究，例如用红细胞进行毒性测定以及与蛋白质和寡核苷酸的相互作用研究，结果表明在所有情况下，它们的毒性都很低，并且与蛋白质和寡核苷酸没有共价相互作用。还测试了螺旋配合物对 MCF-7（人乳腺癌）、A2780（人卵巢癌细胞）、NCI-H460（人肺癌细胞）和 MRC-5（正常人类肺成纤维细胞）的体外细胞毒性，将 IC 值与顺铂进行了比较。我们将尝试证明配体前体的末端取代基是否会对锌螺旋配合物的毒性或抗肿瘤活性产生任何影响。
