Cellular uptake, cytotoxicity, and metabolic profiling of human cancer cells treated with ruthenium(II) polypyridyl complexes [Ru(bpy)2(N--N)]Cl2 with N--N=bpy, phen, dpq, dppz, and dppn |
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Authors: | Schatzschneider Ulrich Niesel Johanna Ott Ingo Gust Ronald Alborzinia Hamed Wölfl Stefan |
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Affiliation: | 1. Lehrstuhl für Anorganische Chemie I – Bioanorganische Chemie, Ruhr‐Universit?t Bochum NC 3/74, Universit?tsstr. 150, 44801 Bochum (Germany), Fax: (+49)?234‐32‐14378;2. Institut für Pharmazie, Freie Universit?t Berlin, K?nigin‐Luise‐Str. 2+4, 14195 Berlin (Germany), Fax: (+49)?30‐838‐56906;3. Institut für Pharmazie und Molekulare Biotechnologie – Abteilung Biologie, Ruprecht‐Karls‐Universit?t Heidelberg, Im Neuenheimer Feld 346, 69120 Heidelberg (Germany), Fax: (+49)?6221‐54‐4884 |
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Abstract: | A series of five ruthenium(II) polypyridyl complexes Ru(bpy)2(N--N)]Cl2 was tested against human HT-29 and MCF-7 cancer cell lines. Cellular uptake efficiency and cytotoxicity were found to increase with the size of the aromatic surface area of the N--N ligand. The most active compound carrying the dppn ligand exhibits a low micromolar IC(50) value against both cell lines comparable to that of cisplatin under similar conditions. Continuous measurement of oxygen consumption, extracellular acidification rate, and impedance of the cell layer with a chip-based sensor system upon exposure to the complexes showed only small changes for the first two parameters throughout the series. A significant and irreversible decrease in impedance was, however, found for the dppn compound. This suggests that its biological activity is related to modifications in cell morphology or cell-cell and cell-matrix contacts. |
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Keywords: | anticancer agents bioinorganic chemistry biological activity studies ruthenium |
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