20.500.12556/RUL-136344 Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes 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 library 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 considered: (i) organoruthenium(II) complexes with p-cymene as an arene ligand, and (ii) organoruthenium(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. cholinesterase enzyme inhibition glutathione S-transferase organoruthenium complex pyrithione β-diketone carbonyl glutathione transferase true false true Angleški jezik Ni določen Članek v reviji 2022-04-25 13:09:16 2022-04-25 13:09:16 2022-09-15 04:13:47 0000-00-00 00:00:00 2021 0 0 16 str. iss. 9, art. 1243 Vol. 9 2021 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 636.09:612 2227-9059 10.3390/biomedicines9091243 76757507 biomedicines-09-01243-v2.pdf biomedicines-09-01243-v2.pdf 1 EEC28853A00B56ECE9BC6CA24F8FBB6E 9e16b5355b491a453ff5157c9b6b009f08524cb464934f96a50f4d1c1ba0b4a1 551ce7ec-c488-11ec-8aca-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=155937 https://www.mdpi.com/2227-9059/9/9/1243 1 129eb3ee-c488-11ec-8aca-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=155936 Veterinarska fakulteta Biotehniška fakulteta Fakulteta za kemijo in kemijsko tehnologijo 0 0 0