Synthesis,crystal structure,DNA/BSA interaction and in vitro antitumor activity of N-heterocycle Cu(II) and Co(II) complexes |
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| Authors: | Jin’an Zhao Shuangcheng Zhi Huaibin Yu Jin Zhang Junshuai Zhang Jiyong Hu |
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| Affiliation: | 1. College of Chemical and Material Engineering, Henan University of Urban Construction, Henan, P.R. Chinazjinan@zzu.edu.cn;3. College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, P.R. China;4. College of Chemical and Material Engineering, Henan University of Urban Construction, Henan, P.R. China |
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| Abstract: | Investigation of N-heterocycle transition metal complexes has led to the discovery of metal-based antitumor agents. Herein, two binuclear complexes, [Cu(p-4-bmb)(Ac)2]2 (1) and [Co(p-4-bmp)Cl2]2 (2), were prepared and characterized. The interactions of 1 and 2 with calf thymus (CT)-DNA and bovine serum albumin (BSA) were detected by absorbance and emission spectroscopy. The complexes bind to CT-DNA via an intercalative mode and show moderate affinity to BSA. Both complexes exhibited remarkable DNA cleavage activity. The MTT assay demonstrated that 1 exhibited higher cytotoxicity against three human alimentary system carcinoma cell lines compared to 2. Further, a cellular uptake assay demonstrated that 1 can accumulate in the nucleus and mitochondria of SMMC7721 cells to induce DNA damage and mitochondrial dysfunction. Fluorescence staining and flow cytometry analyses revealed that 1 can induce cell death by apoptosis. These findings should promote the development of benzimidazole-based transition metal complexes as novel chemotherapy agents with fewer side effects than conventional antitumor drugs. |
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| Keywords: | Benzimidazole Cu(II)/Co(II) Complexes DNA/BSA Interactions anticancer activity |
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