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CT-DNA/HSA binding interactions and cytotoxicity activity of a new copper(II) complex
Inorganic Chemistry Communications ( IF 3.8 ) Pub Date : 2021-09-13 , DOI: 10.1016/j.inoche.2021.108917
Zhen-Fang Zeng 1 , Qiu-Ping Huang 1 , Jie-Hui Cai 1 , Guang-Jin Zheng 1 , Li-Jin Qin 1 , Qiu-Chan Huang 1 , You-Huan Wei 1
Affiliation  

We designed and synthesized a novel copper (II) complex, [Cu(ambt)2(cnbz)2], using 2-amino-6-methoxybenzothiazole (ambt) and 2-chloro-5-nitrobenzoic acid (cnbz) as ligands. Single-crystal X-ray diffraction (XRD), IR (infrared) spectra along with elemental analysis were employed to characterize its structure. Single-crystal XRD analysis illustrated the copper (II) complex belonged to the triclinic crystal system, space group P-1 and formed mononuclear hexa-coordinated structure. Electronic absorption, fluorescence spectrum and viscosity analysis were employed to assess the binding properties of the complex with CT-DNA (calf thymus DNA), as well as HSA (human serum albumin). The calculated binding constants Ka were 5.89 × 104 M−1 and 3.31 × 106 M−1 for CT-DNA and HSA, respectively, implying that complex [Cu(ambt)2(cnbz)2] displays intercalative bindings with CT-DNA and HSA. It also statically quenched CT-DNA/HSA fluorescence. CCK-8 assay revealed that compared to cisplatin, the complex exerts greater anti-proliferative influence against HepG2, HeLa and A549 cell lines. Flow cytometry revealed that [Cu(ambt)2(cnbz)2] arrested the cycle of HepG2 cells at G0/G1 phase, inducing apoptosis / necrosis. The degree of apoptosis / necrosis and inhibition of cell cycle is dose-, as well as time-dependent.



中文翻译:

新型铜(II)复合物的 CT-DNA/HSA 结合相互作用和细胞毒性活性

我们设计并合成了一种新型铜 (II) 配合物 [Cu(ambt) 2 (cnbz) 2 ],使用 2-氨基-6-甲氧基苯并噻唑 (ambt) 和 2-氯-5-硝基苯甲酸 (cnbz) 作为配体。采用单晶 X 射线衍射 (XRD)、IR (红外) 光谱以及元素分析来表征其结构。单晶XRD分析表明铜(II)配合物属于三斜晶系,空间群P-1,形成单核配位结构。采用电子吸收、荧光光谱和粘度分析来评估复合物与 CT-DNA(小牛胸腺 DNA)以及 HSA(人血清白蛋白)的结合特性。计算的结合常数K aCT-DNA 和 HSA 分别为 5.89 × 10 4 M -1和 3.31 × 10 6 M -1,这意味着复合物 [Cu(ambt) 2 (cnbz) 2 ] 显示出与 CT-DNA 和 HSA 的嵌入结合。它还静态猝灭 CT-DNA/HSA 荧光。CCK-8 测定显示,与顺铂相比,该复合物对 HepG2、HeLa 和 A549 细胞系具有更大的抗增殖影响。流式细胞术显示[Cu(ambt) 2 (cnbz) 2 ]在G0/G1期阻滞HepG2细胞的周期,诱导细胞凋亡/坏死。细胞凋亡/坏死和细胞周期抑制的程度是剂量和时间依赖性的。

更新日期:2021-09-16
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