4-(2-羟基-3-氯)苯基-2,2':6',2"-三联吡啶Cu(Ⅱ)配合物的合成、结构表征及抗肿瘤活性
Synthesis, Structural Characterization and Antitumor Activity of Copper(Ⅱ) Complex of 4-(2-Hydroxy-3-chlorine)phenyl-2,2': 6',2'-terpyridine
作者单位E-mail
钟玉君 广西师范大学化学与药学学院, 省部共建药用资源化学与药物分子工程国家重点实验室, 桂林 541004  
陈振锋 广西师范大学化学与药学学院, 省部共建药用资源化学与药物分子工程国家重点实验室, 桂林 541004 chenzf@gxnu.edu.cn 
梁宏 广西师范大学化学与药学学院, 省部共建药用资源化学与药物分子工程国家重点实验室, 桂林 541004 hliang@gxnu.edu.cn 
摘要: 以4-(2-羟基-3-氯)苯基-2,2':6',2"-三联吡啶(HL)为配体,合成了一种新的铜(Ⅱ)配合物[Cu2μ-L-κO,O)2Cl2](1),并通过红外光谱、电喷雾质谱、元素分析及单晶X射线衍射分析等方法对配合物1进行结构表征。配合物1为双核结构,中心铜(Ⅱ)离子为五配位扭曲四方锥几何构型,每个铜离子与1个Cl-以及来自配体(L-)的2个N原子和2个羟基O原子配位,2个铜(Ⅱ)离子通过羟基的桥联形成双核结构。MTT实验结果表明:配合物1对所选5种癌细胞株表现出不同的抑制活性,尤其是对MGC80-3细胞的抑制作用最明显,抑制率高达(84.30±1.28)%,其IC50值为(3.36±0.43)μmol·L-1。流式细胞术分析结果显示:配合物1能诱导MGC80-3细胞凋亡。在配合物1浓度为4.5 μmol·L-1时,MGC80-3的凋亡百分数为41.4%。此外,配合物1将MGC80-3细胞阻滞于G1期,从而抑制肿瘤细胞的生长。
关键词: 三联吡啶  铜(Ⅱ)配合物  抗肿瘤活性  细胞周期  细胞凋亡
基金项目: 国家自然科学基金(No.21431001)和教育部创新团队项目(No.IRT_16R15)资助
Abstract: A new copper(Ⅱ) complex [Cu2(μ-L-κO,O)2Cl2] (1) with 4-(2-hydroxy-3-chloro)phenyl-2,2':6',2'-tribi-pyridine(HL) as ligand was synthesized and characterized by elemental analysis, NMR, ESI-MS as well as single crystal X-ray diffraction analysis. Complex 1 is a binuclear structure, and the central copper(Ⅱ) is coordinated by one Cl- anion, two N atoms and two hydroxyl O atoms from L- to form five-coordination distorted square-pyramid geometric configurations; two copper centers are bridged by two hydroxyl O atoms. MTT assay was employed to test the inhibitory activities of complex 1 against five selected cancer cell lines. The results showed that inhibition rate of MGC80-3 cells was the highest, reaching(84.30±1.28)%, and its IC50 value was(3.36±0.43) μmol·L-1. Flow cytometry analytical results indicated that complex 1 could induce apoptosis of MGC80-3 cells. Under the complex 1 concentration of 4.5 μmol·L-1, the MGC80-3 cell apoptosis percentage was 42.2%. Complex 1 arrested MGC80-3 cells in G1 phase, thereby inhibiting the growth of tumor cells.
Keywords: tribipyridine  copper(Ⅱ) complex  antitumor activity  cell apoptosis  cell cycle
投稿时间:2019-09-15 修订日期:2019-10-17
摘要点击次数:  233
全文下载次数:  217
钟玉君,陈振锋,梁宏.4-(2-羟基-3-氯)苯基-2,2':6',2"-三联吡啶Cu(Ⅱ)配合物的合成、结构表征及抗肿瘤活性[J].无机化学学报,2019,35(11):2089-2094.
查看全文  查看/发表评论  下载PDF阅读器
Support information: