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Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes
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Orientador(es)
Resumo(s)
Cholinesterases (ChEs) show increased activities in patients with Alzheimer’s disease, and remain one of the main therapeutic targets for treatment of this neurodegenerative disorder. A li-brary of organoruthenium(II) complexes was prepared to investigate the influence of their structural elements on inhibition of ChEs, and on another pharmacologically important group of enzymes, glutathione S-transferases (GSTs). Two groups of organoruthenium(II) compounds were consid-ered: (i) organoruthenium(II) complexes with p-cymene as an arene ligand, and (ii) organoruthe-nium(II) carbonyl complexes as CO-releasing molecules. Eight organoruthenium complexes were screened for inhibitory activities against ChEs and GSTs of human and animal origins. Some compounds inhibited all of these enzymes at low micromolar concentrations, while others selectively inhibited either ChEs or GSTs. This study demonstrates the importance of the different structural elements of organoruthenium complexes for their inhibitory activities against ChEs and GSTs, and also proposes some interesting compounds for further preclinical testing as ChE or GST inhibitory drugs.
Descrição
P4-0053 P1-0207 P1-0175 51852 39077
Palavras-chave
Carbonyl Cholinesterase Enzyme inhibition Glutathione S-transferase Organoruthenium complex Pyrithione β-diketone Medicine (miscellaneous) General Biochemistry,Genetics and Molecular Biology SDG 3 - Good Health and Well-being