Ruthenium(II) Complexes Containing Anti-Inflammatory Drugs as Ligands: Synthesis, Characterization and in vitro Cytotoxicity Activities on Cancer Cell Lines

Author(s):Show less -

Lopes, Junai C. S. ^{[1, 2]} ; Damasceno, Jaqueline L. ^[3] ; Oliveira, Pollyanna F. ^[3] ; Guedes, AdrianaP. M. ^[4] ; Tavares, Denise C. ^[3] ; Deflon, Victor M. ^[5] ; Lopes, Norberto P. ^[6] ; Pivatto, Marcos ^[1] ; Batista, Alzir A. ^[4] ; Maia, Pedro I. S. ^[7] ; Von Poelhsitz, Gustavo ^[1]

Affiliation

^[1] Univ Fed Uberlandia, Dept Quim, BR-38400902 Uberlandia, MG - Brazil

^[2] Inst Fed Norte Minas Gerais, BR-39270000 Pirapora, MG - Brazil

^[3] Univ Franca, BR-14404600 Franca, SP - Brazil

^[4] Univ Fed Sao Carlos, Dept Quim, BR-13561901 Sao Carlos, SP - Brazil

^[5] Univ Fed Sao Carlos, Inst Quim Sao Carlos, BR-13566590 Sao Carlos, SP - Brazil

^[6] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, NPPNS, BR-14040903 Ribeirao Preto, SP - Brazil

^[7] Univ Fed Triangulo Mineiro, Inst Ciencias Nat Exatas & Educ, BR-38064200 Uberaba, MG - Brazil

• Document type: Journal article
• Source: Journal of the Brazilian Chemical Society; v. 26, n. 9, p. 1838-1847, SEP 2015.
• Web of Science Citations: 11

Abstract

The synthesis, characterization and cytotoxic activity of cis-[Ru(dicl)(dppm)2]PF6 and cis-[Ru(ibu)(dppm)2]PF6, (dppm = 1,1-bis(diphenylphosphine)methane; dicl = diclofenac anion and ibu = ibuprofen anion), are described in this work. Complexes were characterized by elemental analysis, Fourier transform infrared spectroscopy (FTIR), UV-Vis, 31P{1H} nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRESIMS). X-ray structure of cis-[Ru(ibu)(dppm)2]PF6 is also described. Preliminary calf thymus DNA (ct-DNA) binding studies were carried out by UV-Vis and viscosity experiments, with results suggesting the existence of electrostatic interactions between ruthenium complexes and ct-DNA. Cytotoxicity assays were carried out on a panel of human cancer cell lines and a human normal cell line. Complexes displayed a high to moderate cytotoxicity with IC50 ranging from 5 to 47 µmol L-1. cis-[Ru(ibu) (dppm)2]PF6 was found to be the most active, with IC50 values lower than cisplatin. The degree of cytotoxicity was maintained for the normal cell line, although cis-[Ru(ibu)(dppm)2]PF6 exhibited a similar selectivity to that of cisplatin but with a higher activity for at least two tumor cell lines which evidences a promising anticancer candidate and selects this complex for further experiments. (AU)

• FAPESP's process: 09/54011-8 - Acquisition of a single-crystal X-ray diffractometer for the structural analysis of small molecules and proteins
• Grantee: Victor Marcelo Deflon
• Support Opportunities: Multi-user Equipment Program