In vitro and in vivo studies into the biological activities of\ud 1,10-phenanthroline, 1,10-phenanthroline-5,6-dione and its copper(II)\ud and silver(I) complexes

摘要

1,10-Phenanthroline (phen, 5), 1,10-phenanthroline-5,6-dione (phendione, 6), [Cu(phendione)3]-\ud(ClO4)2·4H2O (12) and [Ag(phendione)2]ClO4 (13) are highly active, in vitro, against a range of normal\udand cancerous mammalian cells, fungal and insect cell lines, with the metal complexes offering a clear\udenhancement in activity. Cytoselectivity was not observed between the tumorigenic and non-tumorigenic\udmammalian lines. In in vivo tests, using Galleria mellonella and Swiss mice, all four compounds were\udwell tolerated in comparison to the clinical agent, cisplatin. In addition, blood samples taken from the\udSwiss mice showed that the levels of the hepatic enzymes, aspartate aminotransferase (AST) and alanine\udaminotransferase (ALT), remained unaffected. Immunocompromised nude mice showed a much lower\udtolerance to 13 and, subsequently, when these mice were implanted with Hep-G2 (hepatic) and HCT-8\ud(colon) human-derived tumors, there was no influence on tumor growth.