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Doctoral Thesis
DOI
10.11606/T.46.2009.tde-06102009-140313
Document
Author
Full name
Renata Rolim Prudente dos Santos
E-mail
Institute/School/College
Knowledge Area
Date of Defense
Published
São Paulo, 2009
Supervisor
Committee
Silva, Denise de Oliveira (President)
Colquhoun, Alison
Esposito, Breno Pannia
Nikolaou, Sofia
Toma, Henrique Eisi
Title in Portuguese
Metalofármacos de rutênio: síntese, caracterização, atividade frente à linhagem celular K562 e estudos de interação com albumina de soro humano (HSA)
Keywords in Portuguese
Antiinflamatórios não esteróides
Dicroísmo circular e fluorescência
Faines
HSA
K562
Rutênio
Abstract in Portuguese
Este trabalho trata do estudo de complexos de rutênio contendo antiinflamatórios não-esteróides, com o objetivo de contribuir para ampliar as pesquisas na área de potenciais metalofármacos antitumorais. A partir de reações do precursor dimetálico [Ru2(O2CCH3)4Cl] com os fármacos carboxílicos sulindaco (HSulin) e diclofenaco de sódio (NaDiclofen) foram isolados, respectivamente, os correspondentes complexos [Ru2(Sulin)4Cl] e [Ru2(Diclofen)4Cl]. A reação entre o monômero [RuCl2(dmso)4] e o meloxicam (H2Melox) deu origem ao derivado misto [Ru(dmso)2(HMelox)2]. Os compostos foram caracterizados por meio de análise elementar, medidas de condutância molar, medidas de susceptibilidade magnética, espectroscopia de absorção eletrônica UV-VIS-IR, espectroscopia vibracional FTIR e Raman, e estudos de análise térmica (TG/DSC/MS). As interações da albumina de soro humana HSA, importante proteína do plasma, com os complexos obtidos, com o análogo [Ru2(IBP)4Cl] (HIBP = ibuprofeno) e também com os fármacos orgânicos não-complexados foram investigadas empregando-se dicroísmo circular, SDS-Page e fluorescência. A atividade antitumoral dos metalofármacos foi avaliada, através de ensaios com MTT, com base nos seus efeitos citotóxicos para a linhagem celular de leucemia humana K562.
Title in English
Ruthenium metallodrugs of diclofenac, sulindac and meloxicam: synthesis, characterization, activity against K562 cell line and interaction with human serum albumin (HSA)
Keywords in English
Circular dichroism and fluorescence
HSA
K562
Non-steroidal antiinflammatory
Ruthenium
Abstract in English
This work describes the study of ruthenium complexes containing non-steroidal antiinflammatory drugs with the aim of helping to expand the research in the field of potential anticancer metallodrugs. Reactions of the [Ru2(O2CCH3)4Cl] dimetal complex with sulindac (HSulin) and sodium diclofenac (NaDiclofen) carboxylic drugs gave the correspondent complexes [Ru2(Sulin)4Cl] and [Ru2(Diclofen)4Cl], respectively. The reaction between the [RuCl2(dmso)4] monomer and the meloxicam drug (H2Melox) led to the mixed derivative [Ru(dmso)2(HMelox)2]. The compounds were characterized by elemental analysis, molar conductance measurements, magnetic susceptibility, UV-VIS-IR electronic absorption spectroscopy, Raman and FTIR vibrational spectroscopies and by studies of thermal analysis (TG / DSC / MS). The interactions of human serum albumin (HSA), the major plasma protein, with the obtained complexes, the analogous [Ru2(IBP)4Cl] (= HIBP ibuprofen) and also with the noncoordinated organic drugs have been investigated by circular dichroism, SDS-Page and fluorescence. The antitumor activity of the metallodrugs has been evaluated by MTT assays, on the basis of their cytotoxic effects on K562 human leukemia cell line.
 
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Publishing Date
2011-06-09
 
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