DNA interactive and selective anticancer activity studies of copper(II) complexes decorated water-soluble porphyrin

Cancer is one of the diseases that seriously threaten the health of peoples. As a representative of metal drugs, cisplatin has considerable promise for the treatment of cancer. However, side effects are one of major problems for cisplatin due to their poor selectivity for cancer cells. We report here, for the first time, the syntheses of three new water-soluble porphyrin-modified copper(II) complexes Cu-P1, Cu-P2, and Cu-P3. Results from calf thymus DNA (ct-DNA)-binding efficiency tests show that three copper(II) complexes could obviously interact with ct-DNA and Cu-P1 characterized the strongest bound performance. Besides, their function on anticancer against A549, H1975, HepG2, and T47D cells were analyzed, they show the best anticancer activity against lung cancer cells H1975, Cu-P1 exhibited the greatest cytotoxic effect among the series, and the ligand L was less active against cancer cells. Furthermore, the cytotoxicities of ligand L, complexes Cu-P1, Cu-P2, Cu-P3, and cisplatin were further evaluated against the breast cells Hs 578Bst and complexes more negligible cytotoxicity than ligand L and cisplatin. The anticancer mechanism is discussed by flow cytometer. Then, density functional theory (DFT) calculations analysis further proved the biological activities of the target compounds. Therefore, preliminary research suggests that these copper(II) complexes can inhibit human malignancy cells.

Automated summary

The study synthesized three new water-soluble porphyrin-modified copper(II) complexes, which showed strong binding performance to cancer cells, especially Cu-P1. In anticancer tests, Cu-P1 exhibited the best activity against lung cancer cells H1975 and showed lesser cytotoxicity to breast cancer cells. Flow cytometry and DFT calculations further supported the biological activities of these copper(II) complexes against malignancy cells.