Cancer is one of the killers endangering human health and its treatment has always been a focus of the medical community. For anticancer drugs, water‐soluble porphyrin and Schiff bases have always been of interest. We report here three Cu(II)‐based complexes functionalized by water‐soluble cationic porphyrin and hydrazine Schiff base, which were prepared and evaluated for their biological activity. The three Cu(II) complexes all exhibited potent binding affinity to calf thymus DNA, the strongest interaction being between CuP2 and DNA. We studied the cytotoxicity of the complexes and ligands against different types of cancer cells (A549, H‐1975, HepG2 and T47D), results showing the ligands are less cytotoxic; therefore, the anticancer activity of the complexes is improved by complexation. Furthermore, the cytotoxicity of ligands and complexes was also evaluated against the normal cell line Hs 578Bst, complexes showing more negligible cytotoxicity than ligand. Moreover, the cellular uptake of these Cu(II) complexes was investigated using the extraction method and results suggested that CuP2 exhibits the best cellular uptake towards H‐1975 cells. Interestingly, fluorescence microscopy experiments and flow cytometric analysis (cell cycle) were used to further investigate the potent anticancer activities.

中文翻译：

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将水溶性卟啉辅助的Cu（II）配合物应用于DNA结合和选择性抗癌活性

癌症是危害人类健康的杀手之一，其治疗一直是医学界关注的焦点。对于抗癌药物，水溶性卟啉和席夫碱一直很受关注。我们在这里报告了三种由水溶性阳离子卟啉和肼席夫碱官能化的基于Cu（II）的配合物，这些配合物均已制备并对其生物学活性进行了评估。这三种Cu（II）配合物都对小牛胸腺DNA表现出强力的结合亲和力，其中最强的相互作用是CuP2和DNA之间。我们研究了复合物和配体对不同类型的癌细胞（A549，H-1975，HepG2和T47D）的细胞毒性，结果显示，配体的细胞毒性较小。因此，复合物可提高复合物的抗癌活性。此外，还针对正常细胞系Hs 578Bst评估了配体和复合物的细胞毒性，该复合物显示出比配体更可忽略的细胞毒性。此外，使用提取方法研究了这些Cu（II）配合物的细胞摄取，结果表明CuP2对H-1975细胞表现出最佳的细胞摄取。有趣的是，荧光显微镜实验和流式细胞仪分析（细胞周期）被用来进一步研究有效的抗癌活性。