| 喷昔洛韦-铜(Ⅱ)配合物的合成、晶体结构及DNA键合作用 |
| Synthesis, Crystal Structure and DNA Binding of Copper(Ⅱ) Complex of Penciclovir |
| 作者 | 单位 | E-mail | | 刘瑞雪 | 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 | | | 赖德霖 | 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 | | | 邓前军 | 佛山科学技术学院材料科学与能源工程学院, 佛山 528000 | ycliu@gxnu.edu.cn | | 程风杰 | 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 | | | 范兰琼 | 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 | | | 刘延成 | 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 | 1192097240@qq.com |
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| 摘要: 将具有生物活性的铜（Ⅱ）离子与临床抗病毒药物喷昔洛韦（PCV）配位，合成了首个喷昔洛韦的金属配合物[Cu（PCV）2（H2O）3]SO4（1），并通过红外光谱、元素分析和X射线单晶衍射分析方法对其结构进行了表征。初步测试了其针对多种典型人肿瘤细胞株的体外抗肿瘤活性。测试结果表明，喷昔洛韦-铜（Ⅱ）配合物1对各种肿瘤细胞株均显示出显著高于喷昔洛韦的增殖抑制活性，其中对于较为敏感的人肝癌细胞BEL-7404，配合物1的增殖抑制活性是喷昔洛韦的3倍以上。进一步，针对抗肿瘤首要靶点DNA，通过紫外-可见吸收光谱、荧光发射光谱以及DNA粘度实验对配合物1与小牛胸腺DNA的键合作用方式进行了探讨。由实验结果推测，DNA应该是配合物1的抗肿瘤活性的重要靶点，其与DNA之间存在典型的插入结合方式。 |
| 关键词: 喷昔洛韦 金属配合物 铜(Ⅱ) 抗肿瘤活性 DNA键合 |
| 基金项目: 国家自然科学基金（No.21561005），广西自然科学基金（No.2017GXNSFDA198048），广东省材料学重点学科开放基金资助项目（No.2017-13）和广西医药产业人才小高地项目（No.1405/1505）资助 |
| Abstract: The first metal complex of the clinical antivirus agent, penciclovir (PCV), was synthesized and structurally characterized by IR, elemental analysis and X-ray single crystal diffraction analysis. In this complex, copper(Ⅱ) was selected as the bioactive metal center, which was coordinated by two PCV molecules to form a new copper(Ⅱ) complex of PCV,[Cu(PCV)2(H2O)3]SO4 (1). The in vitro antitumor activity of complex 1 towards a variety of typical human tumor cell lines has been explored. The results indicated that complex 1 showed enhanced antitumor activity comparing with PCV alone towards all the tested cell lines, in which the human hepatoma cell line BEL-7404 was the most sensitive one to complex 1 (Inhibition ratio (55.83±16.41)%). The inhibitory activity of complex 1 is more than 3 times that of PCV (Inhibition ratio (17.38±5.53)%). Furthermore, the DNA binding mechanism of complex 1 was also studied and discussed by means of UV-Vis absorption and fluorescence emission spectral analyses, as well as the DNA viscosity experiment. The results suggested that DNA, as the primary antitumor target, should be an important binding target of complex 1. And the classic intercalative binding mode might exist between complex 1 and CT-DNA. |
| Keywords: penciclovir metal complex copper (Ⅱ) antitumor activity DNA binding |
| 投稿时间：2018-06-13 修订日期：2018-10-29 |
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| 刘瑞雪,赖德霖,邓前军,程风杰,范兰琼,刘延成.喷昔洛韦-铜(Ⅱ)配合物的合成、晶体结构及DNA键合作用[J].无机化学学报,2019,35(1):125-132. |
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