水溶性铜卟啉配合物的合成、与DNA的相互作用及抗肿瘤活性
Syntheses, DNA-binding and Antitumor Activities of Water Soluble Copper Porphyrins Complexes
作者单位E-mail
哈斯其美格 西北民族大学实验中心, 兰州 730030 ha2qimei@163.com 
陈丽华 西北民族大学实验中心, 兰州 730030  
肖朝虎 西北民族大学实验中心, 兰州 730030  
摘要: 合成了3种水溶性铜卟啉配合物,分别为水溶性含溴铜卟啉(CuP-1)及其溴取代衍生物(CuP-2、CuP-3),并采用核磁氢谱、元素分析、质谱等手段进行了结构表征。利用紫外光谱法、EB-DNA荧光淬灭法、粘度法以及圆二色谱法等光谱法研究了CuP-1、CuP-2和CuP-3与小牛胸腺DNA(CT-DNA)的相互作用。采用噻唑兰(MTT)法,以体外培养的宫颈癌细胞(Hela)和乳腺癌细胞(MDA)为测试细胞株对CuP-1~CuP-3的抗肿瘤活性进行检测。人成纤维细胞(L929)作为正常细胞系。光谱法实验结果表明,CuP-1以插入的方式与CT-DNA相互作用,而CuP-2和CuP-3与CT-DNA以沟面结合的方式相互作用,且CuP-1与CT-DNA的结合能力优于CuP-2和CuP-3。体外抗癌活性实验结果表明,CuP-1~CuP-3对Hela和MDA均有体外抑制细胞增殖作用,呈时间、剂量依赖关系,并且CuP-1的体外抗肿瘤活性明显优于CuP-2、CuP-3。
关键词: 水溶性铜卟啉配合物  小牛胸腺DNA  抗肿瘤活性
基金项目: 甘肃省高等学校科研项目(No.2017B-87)和西北民族大学“一优三特”学科中央高校基本科研业务费(No.31920170168)资助。
Abstract: Three water-soluble copper porphyrin complexes (water-soluble bromine-containing copper porphyrin CuP-1 and its bromine substituted derivatives CuP-2 and CuP-3) have been synthesized and characterized by 1H NMR, elementary analysis and MS spectra. The interaction of CuP-1, CuP-2 and CuP-3 with CT-DNA have been investigated by UV spectrum, EB-DNA fluorescence quenching, viscosity method and circular dichroism spectrum. Moreover, the antitumor activities of CuP-1~CuP-3 against Hela (cervical cancer) cell lines and MDA (breast carcinoma) cell lines have been studied by MTT assay. L929 (human fibroblast) cell line was used as a normal cell lines. Various spectroscopic approaches indicates that CuP-1 could effectively bind with CT-DNA through intercalation mode, while CuP-2 and CuP-3 may interact with CT-DNA by outside groove binding mode. And the binding affinity of CuP-1 with CT-DNA is better than its derivatives CuP-2 and CuP-3. In vitro antitumor activity experiments showed that CuP-1~CuP-3 can inhibit the growth of Hela and MDA cell lines, and the inhibition shows concentration and time dependent. In addition, antitumor activity in vitro of CuP-1 is much better than CuP-2 and CuP-3.
Keywords: water soluble copper porphyrins complexes  CT-DNA  anticancer activity
投稿时间:2018-05-28 修订日期:2018-07-23
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哈斯其美格,陈丽华,肖朝虎.水溶性铜卟啉配合物的合成、与DNA的相互作用及抗肿瘤活性[J].无机化学学报,2018,34(10):1841-1850.
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