Investigation of the pharmacological profiles of dinuclear metal complexes as novel, potent and selective cytotoxic agents against leas-transformed cells


Bostancioglu R. B., Koparal A. T., BENKLİ K.

ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY, vol.37, no.3, pp.897-906, 2014 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 37 Issue: 3
  • Publication Date: 2014
  • Doi Number: 10.1016/j.etap.2014.03.003
  • Journal Name: ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.897-906
  • Keywords: Au(III), Ru(II), Pt(II), Antitumoral activity, Apoptosis, Selective toxicity, RAT EMBRYO CELLS, H-RAS, PLATINUM(II) COMPLEXES, METASTATIC PHENOTYPE, DNA FRAGMENTATION, INDUCE APOPTOSIS, PT(II) COMPLEXES, CANCER-CELLS, A549 CELLS, IN-VITRO
  • Anadolu University Affiliated: Yes

Abstract

Around the world scientists try to design successful cures against still incurable diseases, especially cancers. New targets for prevention and new agents for therapy need to be identified. We synthesized novel metal complexes [Au(L1)(L2)Pt]Cl2 and [Ru(L1)2(L2)Pt]Cl2 for determining their cytotoxic and apoptotic effects. The complexes are synthesized by using 1,8-diaminonaphthalene (L1), and bis-1,4-di[([1,10]phenanthroline-5-il)aminomethyl]cyclohexane (L2) as ligands. This is the first study to examine these metals and these molecules in cancer treatment. We elucidated the effects of test compounds with embryonic rat fibroblast-like cells (F2408) and H-ras oncogene activated embryonic rat fibroblast-like cancer cells (5RP7). Results showed that our complexes are more effective than cisplatin to kill ras-transformed cells. Although the [Au(L1)(L2)Pt]Cl2 compound showed a cytotoxic potency higher than [Ru(L1)2(L2)Pt]Cl2 against cancer cells, it proved to be almost five times less effective in decreasing cell viability over healthy cells. Au(III) compound selectively targets the cancer cells but not the healthy cells. (C) 2014 Elsevier B.V. All rights reserved.