Laboratory of Materials for Electrotechnics, Department of Electrical and Computer Engineering, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece and Institute of Biosciences & Applications, National Centre for Scientific Research "Demokritos", 15310 Athens, Greece.
Institute of Biosciences & Applications, National Centre for Scientific Research "Demokritos", 15310 Athens, Greece.
Dalton Trans. 2020 Feb 25;49(8):2734-2746. doi: 10.1039/c9dt04540f.
Chemotherapeutic metal-based compounds are effective anticancer agents; however, their cytotoxic profile and significant side effects limit their wide application. Natural products, especially flavonoids, are a prominent alternative source of anticancer agents that can be used as ligands for the generation of new bioactive complexes with metal ions of known biochemical and pharmacological activities. Herein, we present the synthesis and detailed structural and physicochemical characterizations of three novel complex assemblies of Ga(iii) with the flavonoid chrysin and the ancillary aromatic chelators 1,10-phenanthroline, 2,2'-bipyridine and imidazole. The complexes constitute the only crystallographically characterized structures having a metal core from the boron group elements and a flavonoid as the ligand. The in vitro biological evaluation of the three complexes in a series of cancer cell lines of different origin established their cytotoxicity and ROS generating potential. In particular, the Ga(iii)-chrysin-imidazole complex displayed the highest anticancer efficacy against all cancer cell lines with IC50 values in the low micromolar range (<1.18 μM), a result worth further investigation.
化疗金属基化合物是有效的抗癌药物;然而,它们的细胞毒性特征和显著的副作用限制了它们的广泛应用。天然产物,特别是类黄酮,是抗癌药物的一个突出的替代来源,可以作为配体用于生成具有已知生化和药理活性的金属离子的新的生物活性配合物。在此,我们介绍了三种新型 Ga(iii)配合物的合成及详细的结构和物理化学特性,这些配合物与黄酮类化合物白杨素和辅助芳香螯合剂 1,10-菲咯啉、2,2'-联吡啶和咪唑。这些配合物构成了唯一的晶体结构,其金属核来自硼族元素,配体为黄酮类化合物。三种配合物在一系列不同来源的癌细胞系中的体外生物学评价确立了它们的细胞毒性和 ROS 生成潜力。特别是 Ga(iii)-白杨素-咪唑配合物对所有癌细胞系表现出最高的抗癌功效,IC50 值在低微摩尔范围内(<1.18 μM),这一结果值得进一步研究。