Institute of Biosciences & Applications, National Centre for Scientific Research "Demokritos", 15310 Athens, Greece; Laboratory of Biochemistry, Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece.
Laboratory of Biochemistry, Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece.
J Inorg Biochem. 2020 Jul;208:111083. doi: 10.1016/j.jinorgbio.2020.111083. Epub 2020 Apr 14.
Curcumin and quercetin are two of the most prominent natural polyphenols with a diverse spectrum of beneficial properties, including antioxidant, anti-inflammatory, chemopreventive and chemotherapeutic activity. The complexation of these natural products with bioactive transition metal ions can lead to the generation of novel metallodrugs with enhanced biochemical and pharmacological activities. Within this framework, the synthesis and detailed structural and physicochemical characterization of two novel complex assemblies of Cu(II) with curcumin and quercetin and the ancillary aromatic chelator 2,2'-bipyridine is presented. The two complexes represent the only crystallographically characterized structures with Cu(II) as the central metal ion and curcumin or quercetin as the ligands. The new complexes were biologically evaluated in vitro for their antioxidant potential, both exhibiting strong scavenging activity in the 2,2-diphenyl-1-picrylhydrazyl assay, and their plasmid DNA binding/cleavage properties. Both complexes appear to be non-toxic in the eukaryotic experimental model Saccharomyces cerevisiae and merit further investigation of their pharmacological profile.
姜黄素和槲皮素是两种最突出的天然多酚,具有广泛的有益特性,包括抗氧化、抗炎、化学预防和化学治疗活性。这些天然产物与生物活性过渡金属离子的络合可以导致具有增强的生化和药理活性的新型金属药物的产生。在这个框架内,介绍了两种新型配合物的合成和详细的结构和物理化学表征,这些配合物由 Cu(II)与姜黄素和槲皮素以及辅助芳香螯合剂 2,2'-联吡啶组成。这两个配合物代表了仅有的以 Cu(II)为中心金属离子和姜黄素或槲皮素为配体的晶体化学表征结构。新的配合物在体外进行了抗氧化潜力的生物学评价,在 2,2-二苯基-1-苦基肼测定中均表现出很强的清除活性,并且具有质粒 DNA 结合/切割性质。这两种配合物在真核实验模型酿酒酵母中似乎没有毒性,值得进一步研究其药理特性。