Forty Years after the Discovery of Its Nucleolytic Activity: [Cu(phen)2]2+ Shows Unattended DNA Cleavage Activity upon Fluorination,Chemistry - A European Journal

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Forty Years after the Discovery of Its Nucleolytic Activity: [Cu(phen)2]2+ Shows Unattended DNA Cleavage Activity upon Fluorination
Chemistry - A European Journal ( IF 3.9 ) Pub Date : 2020-11-27 , DOI: 10.1002/chem.202004594
Carsten Lüdtke ₁ , Sebastian Sobottka ₁ , Julian Heinrich ₂ , Phil Liebing ₂ , Stefanie Wedepohl ₃ , Biprajit Sarkar _{1,

4} , Nora Kulak _{1,

2}

Affiliation

[Cu(phen)₂]²⁺ (phen=1,10‐phenanthroline) is the first and still one of the most efficient artificial nucleases. In general, when the phen ligand is modified, the nucleolytic activity of its Cu^II complex is significantly reduced. This is most likely due to higher steric bulk of such ligands and thus lower affinity to DNA. Cu^II complexes with phen ligands having fluorinated substituents (F, CF₃, SF₅, SCF₃) surprisingly showed excellent DNA cleavage activity—in contrast to the unsubstituted [Cu(phen)₂]²⁺—in the absence of the otherwise required classical, bioabundant external reducing agents like thiols or ascorbate. This nucleolytic activity correlates well with the half‐wave potentials E_1/2 of the complexes. Cancer cell studies show cytotoxic effects of all complexes with fluorinated ligands in the low μm range, whereas they were less toxic towards healthy cells (fibroblasts).

中文翻译：

发现其核酸分解活性后四十年：[Cu（phen）2] 2+显示氟化后无人看管的DNA裂解活性。

[Cu（phen）₂ ] ²⁺（phen = 1,10-phenothroline）是第一个也是最有效的人工核酸酶之一。通常，当对phen配体进行修饰时，其Cu ^II复合物的溶核活性会大大降低。这很可能是由于这类配体的空间体积较大，因此对DNA的亲和力较低。具有未取代的[F（CF ₃，SF ₅，SCF ₃）取代基的phen配体的Cu ^II配合物与未取代的[Cu（phen）₂ ]相比，具有出色的DNA裂解活性。²⁺ -在没有其他必要的经典生物富集外部还原剂（如硫醇或抗坏血酸）的情况下。这种核酸分解活性与复合物的半波电势E _1/2密切相关。癌细胞研究表明，所有复合物均具有低μm范围内的氟化配体，但对健康细胞（成纤维细胞）的毒性较小。

更新日期：2020-11-27

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