Gan Qian, Fu Xiabing, Chen Weijiang, Xiong Yahong, Fu Yinlian, Chen Shi, Le Xueyi
Department of Applied Chemistry, South China Agricultural University, Guangzhou, 510642, People's Republic of China.
Department of Applied Mathematics, South China Agricultural University, Guangzhou, 510642, People's Republic of China.
J Fluoresc. 2016 May;26(3):905-18. doi: 10.1007/s10895-016-1779-2. Epub 2016 Mar 9.
A new mixed ligand copper(II)-dipeptide complex with 2-(2'-pyridyl)benzothiazole (pbt), [Cu(Gly-L-leu)(pbt)(H2O)]·ClO4 (Gly-L-leu = Glycyl-L-leucine anion) was synthesized and characterized by various physico-chemical means. The DNA binding and cleavage properties of the complex investigated by viscosity, agarose gel electrophoresis and multi-spectroscopic techniques (UV, circular dichroism (CD) and fluorescence) showed that the complex was bound to CT-DNA through intercalation mode with moderate binding constant (K b = 3.132 × 10(4) M(-1)), and cleaved pBR322 DNA efficiently (~ 5 μM) in the presence of Vc, probably via an oxidative mechanism induced by •OH. Additionally, the interaction of the complex with human serum albumin (HSA) was explored by UV-visible, CD, fluorescence, synchronous fluorescence and 3D fluorescence spectroscopy. The complex exhibits desired affinity to HSA through hydrophobic interaction. Moreover, the cytotoxicity of the complex against three human carcinoma cell lines (HeLa, HepG2 and A549) was evaluated by MTT assay, which showed that the complex had effective cytotoxicity and higher inhibition toward A549 cell lines with IC50 of 38.0 ± 3.2 μM.
合成了一种新的含2-(2'-吡啶基)苯并噻唑(pbt)的混合配体铜(II)-二肽配合物[Cu(Gly-L-leu)(pbt)(H2O)]·ClO4(Gly-L-leu = 甘氨酰-L-亮氨酸阴离子),并通过多种物理化学方法对其进行了表征。通过粘度、琼脂糖凝胶电泳和多光谱技术(紫外、圆二色性(CD)和荧光)研究了该配合物的DNA结合和切割特性,结果表明该配合物通过插入模式与CT-DNA结合,结合常数适中(Kb = 3.132×10(4) M(-1)),并且在Vc存在下能有效切割pBR322 DNA(约5 μM),可能是通过•OH诱导的氧化机制。此外,通过紫外可见光谱、CD光谱、荧光光谱、同步荧光光谱和三维荧光光谱研究了该配合物与人血清白蛋白(HSA)的相互作用。该配合物通过疏水相互作用对HSA表现出预期的亲和力。此外,通过MTT法评估了该配合物对三种人类癌细胞系(HeLa、HepG2和A549)的细胞毒性,结果表明该配合物具有有效的细胞毒性,对A549细胞系的抑制作用更强,IC50为38.0±3.2 μM。