Synthesis,Characterization, DNA/HSA Interactions,and Anticancer Activity of Two Novel Copper(II) Complexes with 4-Chloro-3-Nitrobenzoic Acid Ligand |
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| Authors: | Zhen-Fang Zeng Qiu-Ping Huang Jie-Hui Cai Guang-Jin Zheng Qiu-Chan Huang Zi-Lu Liu Zi-Lu Chen You-Huan Wei |
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| Institution: | 1.School of Chemical and Biological Engineering, Guangxi Normal University for Nationalities, 23 Fozi Road, Chongzuo 532200, China; (Q.-P.H.); (J.-H.C.); (G.-J.Z.); (Q.-C.H.); (Z.-L.L.);2.State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, 15 Yucai Road, Guilin 541004, China |
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| Abstract: | The purpose of this study was to identify new metal-based anticancer drugs; to this end, we synthesized two new copper(II) complexes, namely Cu(ncba)4(phen)] (1) and Cu(ncba)4(bpy)] (2), comprised 4-chloro-3-nitrobenzoic acid as the main ligand. The single-crystal XRD approach was employed to determine the copper(II) complex structures. Binding between these complexes and calf thymus DNA (CT-DNA) and human serum albumin (HSA) was explored by electronic absorption, fluorescence spectroscopy, and viscometry. Both complexes intercalatively bound CT-DNA and statically and spontaneously quenched DNA/HSA fluorescence. A CCK-8 assay revealed that complex 1 and complex 2 had substantial antiproliferative influences against human cancer cell lines. Moreover, complex 1 had greater antitumor efficacy than the positive control cisplatin. Flow cytometry assessment of the cell cycle demonstrated that these complexes arrested the HepG2 cell cycle and caused the accumulation of G0/G1-phase cells. The mechanism of cell death was elucidated by flow cytometry-based apoptosis assays. Western blotting revealed that both copper(II) complexes induced apoptosis by regulating the expression of the Bcl-2(Bcl-2, B cell lymphoma 2) protein family. |
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| Keywords: | anticancer apoptosis copper(II) complex cytotoxicity DNA/HSA |
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