Publication Type Journal Article
Title Antitumour and Toxicity Evaluation of a Ru(II)-Cyclopentadienyl Complex in a Prostate Cancer Model by Imaging Tools
Authors Lurdes Gano Teresa Pinheiro Antonio P. Matos Francisco Tortosa Tiago F. Jorge Maria S. Goncalves Marta Martins Tânia S. Morais Andreia Valente Ana Isabel Tomaz Maria H. Garcia Fernanda M. Marques
Groups BIOIN
Journal ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
Year 2019
Month
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Volume 19
Number 10
Pages 1262-1275
Abstract Background: Ruthenium complexes have been extensively investigated for their prospective value as alternatives to cisplatin. Recently, we reported the in vitro anticancer properties of a family of organometallic ruthenium(II)-cyclopentadienyl complexes and have explored their mechanism of action. Objective: The purpose of this study was to evaluate the in vivo antitumour efficacy and toxicity of one of these Ru(II) compounds, [RuCp(mTPPMSNa)(2,2 -bipy)][CF3SO2] (TM85) which displayed an interesting spectrum of activity against several cancer cells. Methods: Studies to assess the antitumour activity and toxicity were performed in a metastatic prostate (PC3) mice model using ICP-MS, nuclear microscopy, elemental analysis and Transmission Electron Microscopy (TEM). Results: TM85 showed low systemic toxicity but no significant tumour reduction, when administered at tolerated dose (20mg/kg) over 10 days. Ru was mainly retained in the liver and less in kidneys, with low accumulation in tumour. Increased bilirubin levels, anomalous Ca and Fe concentrations in liver and mitochondria alterations were indicative of liver injury. The hepatotoxicity observed was less severe than that of cisplatin and no nephrotoxicity was found. Conclusion: Under the experimental conditions of this study, TM85 is less toxic than cisplatin, induces similar tumour reduction and avoids the formation of metastatic foci. No renal toxicity was observed by the analysis of creatinine levels and the effective renal plasma flow by Tc-99m-MAG3 clearance. Hence, it can be considered a valuable compound for further studies in the field of Ru-based anticancer drugs.
DOI http://dx.doi.org/10.2174/1871520619666190318152726
ISBN
Publisher
Book Title
ISSN 1871-5206
EISSN 1875-5992
Conference Name
Bibtex ID ISI:000492763600007
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