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两种双麦芽酚多胺:其钯 (II) 配合物的合成、表征和研究,探索其潜在的抗癌活性。

Two bis-maltol-polyamines: Synthesis, characterization and studies of their palladium(II) complexes exploring their potential anticancer activity.

发表日期:2024 Oct 09
作者: Daniele Paderni, Eleonora Macedi, Enrica Sordini, Stefano Amatori, Patrizia Rossi, Mauro Formica, Luca Giorgi, Paola Paoli, Mirco Fanelli, Vieri Fusi
来源: JOURNAL OF INORGANIC BIOCHEMISTRY

摘要:

对双麦芽酚多胺家族(特别是 Malten 和 Maltonis)所表现出的抗肿瘤和结合特性的兴趣促使我们从生物学和金属受体的角度研究后者的 Pd2 复合物。 X 射线衍射证实,Malten-Pd2 复合物可以将 Sr2 等硬物质容纳在其配位驱动的预组织口袋中。 UV-Vis 和 NMR 数据表明,即使在酸性 pH 值下,Malten-Pd2 也会形成,并且存在于各种 pH 值的水溶液中。单核复合物足够稳定,不会在溶液中长时间(至少一周)释放 Pd2,因此 Malten-Pd2 与 Maltonis-Pd2 类似,适合在生物分析中进行测试。对 U937 细胞系的研究表明,Malten 诱导的细胞存活率降低的作用在 Malten-Pd2 中部分消失,而 Maltonis-Pd2 和 Maltonis 的作用之间没有监测到差异,这表明游离麦芽酚部分的可用性,保留在 Maltonis-Pd2 中,但不保留在 Malten-Pd2 中,这对于保证这些化合物的生物活性至关重要。版权所有 © 2024 作者。由爱思唯尔公司出版。保留所有权利。
The interest in the antineoplastic and binding properties shown by the bis-maltol polyamine family, particularly Malten and Maltonis, prompted us to study the Pd2+ complexes of these latter from both a biological and metallo-receptor point of view. The Malten-Pd2+ complex can lodge hard species such as Sr2+ in its coordination-driven preorganized pocket, as confirmed by X-ray diffraction. UV-Vis and NMR data showed that Malten-Pd2+ forms even at acidic pH and exists in aqueous solution in a wide range of pH. The mononuclear complex is stable enough not to release Pd2+ in solution for a long period of time (at least one week), thus Malten-Pd2+, similarly to Maltonis-Pd2+, is suitable to be tested in biological analyses. Studies on the U937 cell line revealed that the effect on cell survival reduction induced by Malten is partially lost in Malten-Pd2+, while no differences where monitored between the effects of Maltonis-Pd2+ and Maltonis, suggesting that the availability of free maltol moieties, that is retained in Maltonis-Pd2+, but not in Malten-Pd2+, is crucial to guarantee the biological activity of these compounds.Copyright © 2024 The Authors. Published by Elsevier Inc. All rights reserved.