研究动态
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含有腙和联吡啶/菲咯啉配体的铜(II)络合物,用于抗乳腺癌细胞的抗癌应用。

Copper(II) complexes containing hydrazone and bipyridine/phenanthroline ligands for anticancer application against breast cancer cells.

发表日期:2024 Oct 12
作者: Dorothy Priyanka Dorairaj, Prashant Kumar, Haritha Rajasekaran, Nattamai Bhuvanesh, Sodio C N Hsu, Ramasamy Karvembu
来源: JOURNAL OF INORGANIC BIOCHEMISTRY

摘要:

在这项工作中,合成了含有腙和联吡啶配体(CB1-CB5)或腙和菲咯啉配体(CP1-CP5)的混合配体Cu(II)配合物,并通过光谱和分析技术进行了表征。配合物CB1的单晶X射线结构表明,联吡啶的两个氮原子、一个羰基氧、一个甲亚碱氮和一个腙配体的羟基氧与Cu(II)离子配位,采用扭曲的四角锥几何形状。通过吸收和发射研究分析了这些复合物与小牛胸腺 (CT) DNA 和牛血清白蛋白 (BSA) 的相互作用。此外,专门针对乳腺癌细胞(即 MCF7、T47D 和 MDA MB 231)以及正常乳腺 MCF 10a 细胞系研究了复合物的体外抗癌活性。从 IC50 值可以看出,带有菲咯啉的配合物 (CP1-CP5) 比其联吡啶对应物表现出更好的活性。此外,通过吖啶橙/溴化乙锭 (AO/EB)、4',6-二脒基-2-,研究了对 T47D 癌细胞的 IC50 值为 5.8 ± 0.3 μM 的最活跃复合物 CP1 的细胞死亡模式。苯基吲哚 (DAPI) 和膜联蛋白-V 异硫氰酸荧光素 (FITC) 染色测定显示细胞凋亡。最后,细胞周期分析表明,复杂的 CP1 会诱导 G0/G1 期 T47D 癌细胞死亡。版权所有 © 2024 Elsevier Inc. 保留所有权利。
In this work, mixed ligand Cu(II) complexes containing hydrazone and bipyridine ligands (CB1-CB5), or hydrazone and phenanthroline ligands (CP1-CP5) have been synthesized and characterized by spectroscopic and analytical techniques. Single crystal X-ray structure of complex CB1 revealed that two nitrogen atoms from bipyridine, one carbonyl oxygen, one azomethine nitrogen and one hydroxyl oxygen from the hydrazone ligand coordinated to Cu(II) ion, adopting a distorted square pyramidal geometry. Interaction of these complexes with calf thymus (CT) DNA and bovine serum albumin (BSA) was analyzed by absorption and emission studies. Further, the in vitro anticancer activity of the complexes was investigated exclusively against the breast cancer cells namely MCF7, T47D and MDA MB 231, and a normal breast MCF 10a cell line. The phenanthroline bearing complexes (CP1-CP5) displayed better activity than their bipyridine counterparts as seen from the IC50 values. In addition, the most active complex CP1 having an IC50 value of 5.8 ± 0.3 μM against T47D cancer cells was investigated for its mode of cell death through acridine orange/ethidium bromide(AO/EB), 4',6-diamidino-2-phenylindole (DAPI) and Annexin-V fluorescein isothiocyanate (FITC) staining assays which revealed apoptosis. Lastly, the cell cycle analysis revealed that complex CP1 induced cell death in T47D cancer cells at the G0/G1 phase.Copyright © 2024 Elsevier Inc. All rights reserved.