Amalia García-García, Pablo Cristobal-Cueto, Tania Hidalgo, Iñigo J. Vitórica-Yrezábal, Antonio Rodríguez-Diéguez, Patricia Horcajada, Sara Rojas
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引用次数: 0
摘要
我们获得了两种基于 5-nitropicolinate 配体（5-npic）的新型镧系元素络合物，并对其进行了全面表征。单晶 X 射线衍射显示，这些化合物与我们之前发表的一种镝络合物结构相同，都是基于双核单体与扩展氢键网络连接在一起，最终化学式为 [Ln2(5-npic)6(H2O)4]-(H2O)2，其中 Ln = Dy (1)、Gd (2) 和 Tb (3)。初步的光致发光研究表明，所有配合物都具有以配体为中心的发射。这些材料的潜在抗肿瘤活性在前列腺癌细胞系（PC-3；男性第二大常见癌症）中进行了检测，结果显示其具有显著的抗癌活性（500 μg-mL-1时为50-60%）。反过来，复合物及其前体在人类免疫 HL-60 细胞中的生物相容性也很高。鉴于游离的 5-npic 配体（约 40-50%）在肿瘤细胞系中具有最强的毒性作用，该分子的存在似乎触发了复合物的整体抗癌性能。
Potential antiprostatic performance of novel lanthanide-complexes based on 5-nitropicolinic acid
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.
期刊介绍：
Biological inorganic chemistry is a growing field of science that embraces the principles of biology and inorganic chemistry and impacts other fields ranging from medicine to the environment. JBIC (Journal of Biological Inorganic Chemistry) seeks to promote this field internationally. The Journal is primarily concerned with advances in understanding the role of metal ions within a biological matrix—be it a protein, DNA/RNA, or a cell, as well as appropriate model studies. Manuscripts describing high-quality original research on the above topics in English are invited for submission to this Journal. The Journal publishes original articles, minireviews, and commentaries on debated issues.
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