Department of Chemistry, Aligarh Muslim University, Aligarh 202002, UP, India.
Department of Chemistry, Aligarh Muslim University, Aligarh 202002, UP, India.
Int J Biol Macromol. 2024 Jan;254(Pt 1):127521. doi: 10.1016/j.ijbiomac.2023.127521. Epub 2023 Oct 26.
New Quercetin-phenylalanine metal-based therapeutic agents of the formulation [Qu(Phe)M(II).(HO)].NO where M(II) = Co(II) and Ni(II) and [Qu(Phe)Cu(II).(HO)] were synthesized and their structure was predicted by IR, UV-vis, EPR and ESI-MS spectroscopic techniques. The bio-molecular interaction studies of the Quercetin-phenylalanine complexes, 1-3 with ct-DNA and BSA were performed using a battery of complimentary biophysical techniques. The corroborative results of these experiments revealed strong binding propensity via electrostatic interactions probably through minor grove binding towards ct-DNA, therapeutic target. The binding affinity of Quercetin-phenylalanine complexes 1-3 was quantified by determining binding constants values, K, K, and the magnitude of binding propensity followed the order 3 > 1 > 2, implicating the preferential binding of Cu(II) complex 3 with ct-DNA. The cleavage studies were performed with complexes using gel electrophoretic mobility assay. The complexes 1-3 demonstrated efficient cleaving ability by the hydrolytic cleavage pathway involving hydroxyl (OH) radicals. BSA binding profile of Quercetin-phenylalanine metal therapeutics 1-3 was studied in order to understand the drug carrier potential of these compounds and found that complex 3 was capable of binding preferentially with BSA as compared to other complexes.
合成了 [Qu(Phe)M(II).(HO)].NO 形式的新型槲皮素-苯丙氨酸金属治疗剂,其中 M(II) = Co(II) 和 Ni(II),[Qu(Phe)Cu(II).(HO)],并通过 IR、UV-vis、EPR 和 ESI-MS 光谱技术预测了其结构。使用一系列互补的生物物理技术研究了 Quercetin-phenylalanine 配合物 1-3 与 ct-DNA 和 BSA 的生物分子相互作用。这些实验的协同结果表明,通过静电相互作用具有很强的结合倾向,可能通过小沟结合对治疗靶标 ct-DNA 具有亲和力。通过确定结合常数值 K、K 和结合倾向的大小定量了 Quercetin-phenylalanine 配合物 1-3 的结合亲和力,其顺序为 3>1>2,表明 Cu(II)配合物 3 与 ct-DNA 的优先结合。使用凝胶电泳迁移率测定法进行了配合物的切割研究。配合物 1-3 通过涉及羟基 (OH) 自由基的水解切割途径表现出有效的切割能力。为了了解这些化合物的药物载体潜力,研究了 Quercetin-phenylalanine 金属治疗剂 1-3 的 BSA 结合谱,发现与其他配合物相比,配合物 3 能够优先与 BSA 结合。