School of Chemistry and Physics, University of KwaZulu-Natal, Pietermaritzburg, South Africa.
Biomedical Biotechnology Research Unit, Department of Biochemistry and Microbiology, Rhodes University, Grahamstown, South Africa.
J Biomol Struct Dyn. 2021 Jul;39(11):4077-4088. doi: 10.1080/07391102.2020.1775126. Epub 2020 Jun 11.
Deoxyribonucleic acid (DNA) and bovine serum albumin (BSA) binding interactions for a series of ruthenium heterocyclic complexes were monitored using ultraviolet-visible (UV-Vis) spectrophotometry, fluorescence emission spectroscopy and agarose gel electrophoresis. Investigations of the DNA interactions for the metal complexes revealed that they are groove-binders with intrinsic binding constants in the order of 10 - 10 . Electronic spectrophotometric DNA titrations of the -heterocyclic metal complexes illustrated hypochromism of their intraligand electronic transitions and the presence of diffuse isosbestic points which are synonymous with homogeneous binding modes. Metal complexes with the -heterocyclic chelates also showed alterations in their intraligand transitions and changes in their metal-based electronic transitions which are suggestive of metal coordination to the CT-DNA structure. Using agarose gel electrophoresis assessments, Hoechst DNA binding competition studies corroborate that the metal complexes are DNA groove-binders. Optimal uptake of these metal complexes by BSA was observed based on their optimal apparent association and Stern-Volmer constants (K and K > 10 ). Radical scavenging studies revealed that the metal complexes have high activities towards the neutralization of NO and DPPH radicals. Data attained from the BSA electronic spectrophotometric titrations for the majority of the metal complexes illustrated distinct hyperchromism accompanied with blue shifts which indicates unwinding of the protein strands. Predominately, the metal complexes showed moderate cytotoxicity against both triple-negative breast cancer and cervical cancer cell lines that was greater than that of 5-fluorouracil.Communicated by Ramaswamy H. Sarma.
脱氧核糖核酸（DNA）和牛血清白蛋白（BSA）与一系列钌杂环配合物的结合相互作用通过紫外-可见（UV-Vis）分光光度法、荧光发射光谱法和琼脂糖凝胶电泳进行监测。对金属配合物与 DNA 的相互作用的研究表明，它们是沟结合物，具有 10 - 10 的固有结合常数。-杂环金属配合物的电子分光光度法 DNA 滴定表明其内配位体电子跃迁的减色效应和存在弥散等色点，这与均匀结合模式同义。带有-杂环螯合物的金属配合物也表现出其内配位体跃迁的改变以及其基于金属的电子跃迁的改变，这表明金属与 CT-DNA 结构的配位。通过琼脂糖凝胶电泳评估、Hoechst DNA 结合竞争研究证实，金属配合物是 DNA 沟结合物。基于其最佳表观缔合常数和 Stern-Volmer 常数（K 和 K > 10 ），观察到这些金属配合物对 BSA 的最佳摄取。自由基清除研究表明，金属配合物对中和 NO 和 DPPH 自由基具有高活性。对于大多数金属配合物，BSA 电子分光光度滴定获得的数据表明明显的增色效应伴随着蓝移，这表明蛋白质链的解旋。大多数情况下，金属配合物对三阴性乳腺癌和宫颈癌细胞系的细胞毒性大于 5-氟尿嘧啶。由 Ramaswamy H. Sarma 传达。
