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Cu(II) 配位聚合物通过靶向 BCL-2 蛋白并激活凋亡途径抑制肝癌发展。

Cu(II) Coordination Polymer Inhibits Liver Cancer Development via Targeting BCL-2 Protein and Activating Apoptotic Pathway.

机构信息

Department of Hepatobiliary and Pancreatic Surgery, Wuhan Central Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei, China.

出版信息

Dis Markers. 2021 Oct 12;2021:2174290. doi: 10.1155/2021/2174290. eCollection 2021.

Abstract

In the current study, a Cu(II) coordination polymer (CP) has been created in success with the solvothermal reaction between an asymmetrical rigid N-heterocyclic carboxylatic acid (HL) and Cu(NO)·3HO in the existence of 1,3-Hbdc, the second assistant ligand (in which 1,3-Hbdc is benzene-1,3-dicarboxylic acid and HL is 1-(4-carboxylphenyl)-3-(prazin-2-yl)-1H-1,2,4-triazole), and the chemical composition of this compound is [Cu(L)(1,3-bdc)(HO)]n (). In the biological aspect, we screened the antiproliferation activity of the Cu(II) coordination polymer on five kinds of human cancer cell lines. IC and MTT assay results indicated that complex had a spectral antiproliferative activity against liver cancer cells, peculiarly on human HepG2 liver cancer cells. From the data of Annexin V-FITC/PI assay and ROS detection, we can find that complex exerts an antitumor effect by inducing ROS generation and cell apoptosis. Caspase-3 and caspase-9 activity detection revealed that activation of caspase-3 and caspase-9 plays vital roles in HepG2 cell apoptosis. These outcomes indicate that is an excellent compound in treating cancer.

摘要

在当前的研究中,通过不对称刚性 N-杂环羧酸(HL)与 Cu(NO)·3HO 在 1,3-Hbdc(其中 1,3-Hbdc 是苯-1,3-二羧酸,HL 是 1-(4-羧基苯基)-3-(哒嗪-2-基)-1H-1,2,4-三唑)存在下的溶剂热反应,成功合成了一种 Cu(II)配位聚合物(CP),该化合物的化学式为[Cu(L)(1,3-bdc)(HO)]n ()。在生物学方面,我们筛选了 Cu(II)配位聚合物对五种人类癌细胞系的增殖抑制活性。IC 和 MTT 测定结果表明,配合物对肝癌细胞具有广谱的增殖抑制活性,特别是对人 HepG2 肝癌细胞。从 Annexin V-FITC/PI 检测和 ROS 检测的数据中,我们可以发现配合物通过诱导 ROS 生成和细胞凋亡发挥抗肿瘤作用。Caspase-3 和 caspase-9 活性检测表明 caspase-3 和 caspase-9 的激活在 HepG2 细胞凋亡中起着重要作用。这些结果表明,是一种治疗癌症的优秀化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a168/8958075/056474f300d1/DM2021-2174290.001.jpg

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