关键词: 5-Nitropicolinic acid Coordination compounds Lanthanide Prostate cancer Single-crystal X-ray diffraction

Mesh : Humans Lanthanoid Series Elements / chemistry pharmacology Picolinic Acids / chemistry pharmacology Antineoplastic Agents / pharmacology chemistry Coordination Complexes / chemistry pharmacology chemical synthesis Male Drug Screening Assays, Antitumor Models, Molecular HL-60 Cells Crystallography, X-Ray Molecular Structure Cell Line, Tumor PC-3 Cells Prostatic Neoplasms / drug therapy pathology Cell Survival / drug effects Cell Proliferation / drug effects

来  源:   DOI:10.1007/s00775-024-02054-0   PDF(Pubmed)

Abstract:
Two new lanthanide-complexes based on the 5-nitropicolinate ligand (5-npic) were obtained and fully characterized. Single-crystal X-ray diffraction revealed that these compounds are isostructural to a Dy-complex, previously published by us, based on dinuclear monomers link together with an extended hydrogen bond network, providing a final chemical formula of [Ln2(5-npic)6(H2O)4]·(H2O)2, where Ln = Dy (1), Gd (2), and Tb (3). Preliminary photoluminescent studies exhibited a ligand-centered emission for all complexes. The potential antitumoral activity of these materials was assayed in a prostatic cancer cell line (PC-3; the 2nd most common male cancerous disease), showing a significant anticancer activity (50-60% at 500 μg·mL-1). In turn, a high biocompatibility by both, the complexes and their precursors in human immunological HL-60 cells, was evidenced. In view of the strongest toxic effect in the tumoral cell line provided by the free 5-npic ligand (~ 40-50%), the overall anticancer complex performance seems to be triggered by the presence of this molecule.
摘要:
获得了两种基于5-硝基吡啶甲酸配体(5-npic)的新镧系元素配合物,并对其进行了充分表征。单晶X射线衍射表明,这些化合物与Dy配合物同构,以前由我们出版,基于双核单体与扩展的氢键网络连接在一起,提供[Ln2(5-npic)6(H2O)4]·(H2O)2的最终化学式,其中Ln=Dy(1),Gd(2),Tb(3)。初步的光致发光研究显示,所有配合物都以配体为中心的发射。在前列腺癌细胞系(PC-3;第二常见的男性癌性疾病)中测定了这些材料的潜在抗肿瘤活性,显示出显着的抗癌活性(在500μg·mL-1时为50-60%)。反过来,两者的高生物相容性,人类免疫学HL-60细胞中的复合物及其前体,有证据。鉴于由游离5-npic配体(〜40-50%)提供的肿瘤细胞系中最强的毒性作用,整体抗癌复合物的性能似乎是由该分子的存在引发的。
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