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Novel organoruthenium(II) complex C1 selectively inhibits butyrylcholinesterase without side effects on neuromuscular transmission
ID Trobec, Tomaž (Avtor), ID Žužek, Monika C. (Avtor), ID Sepčić, Kristina (Avtor), ID Kladnik, Jerneja (Avtor), ID Turel, Iztok (Avtor), ID Frangež, Robert (Avtor)

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Izvleček
Enzyme butyrylcholinesterase (BChE) shows increased activity in some brain regions after progression of Alzheimer’s disease and is therefore one of the therapeutic targets for symptomatic treatment of this neurodegenerative disorder. The organoruthenium(II) complex [(η$^6$-p-cymene)Ru(II)(1-hydroxy-3-methoxypyridine-2(1H)-thionato)pta]PF$_6$ (C1) was designed based on the results of our previous structure–activity studies. Inhibitory activity toward cholinesterase enzymes shows that this complex selectively, competitively, and reversibly inhibits horse serum BChE (hsBChE) with an IC$_{50}$ value of 2.88 µM. When tested at supra-pharmacological concentrations (30, 60, 90, and 120 µM), C1 had no significant effect on the maximal amplitude of nerve-evoked and directly elicited single-twitch and tetanic contractions. At the highest tested concentration (120 µM), C1 had no effect on resting membrane potential, but significantly decreased the amplitude of miniature end-plate potentials (MEPP) without reducing their frequency. The same concentration of C1 had no effect on the amplitude of end-plate potentials (EPP), however it shortened the half-decay time of MEPPs and EPPs. The decrease in the amplitude of MEPPs and shortening of the half-decay time of MEPPs and EPPs suggest a possible weak inhibitory effect on muscle-type nicotinic acetylcholine receptors (nAChR). These combined results show that, when applied at supra-pharmacological concentrations up to 120 µM, C1 does not importantly affect the physiology of neuromuscular transmission and skeletal muscle contraction.

Jezik:Angleški jezik
Ključne besede:organoruthenium(II) complex, acetylcholinesterase, butyrylcholinesterase, mouse neuromuscular system, ruthenium, Alzheimer disease, neurodegenerative diseases
Vrsta gradiva:Članek v reviji
Tipologija:1.01 - Izvirni znanstveni članek
Organizacija:VF - Veterinarska fakulteta
BF - Biotehniška fakulteta
FKKT - Fakulteta za kemijo in kemijsko tehnologijo
Status publikacije:Objavljeno
Različica publikacije:Objavljena publikacija
Leto izida:2023
Št. strani:14 str.
Številčenje:Vol. 24, iss. 3, art. 2681
PID:20.500.12556/RUL-144178 Povezava se odpre v novem oknu
UDK:616-092
ISSN pri članku:1422-0067
DOI:10.3390/ijms24032681 Povezava se odpre v novem oknu
COBISS.SI-ID:140487427 Povezava se odpre v novem oknu
Datum objave v RUL:02.02.2023
Število ogledov:1142
Število prenosov:105
Metapodatki:XML DC-XML DC-RDF
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Gradivo je del revije

Naslov:International journal of molecular sciences
Skrajšan naslov:Int. j. mol. sci.
Založnik:MDPI
ISSN:1422-0067
COBISS.SI-ID:2779162 Povezava se odpre v novem oknu

Licence

Licenca:CC BY 4.0, Creative Commons Priznanje avtorstva 4.0 Mednarodna
Povezava:http://creativecommons.org/licenses/by/4.0/deed.sl
Opis:To je standardna licenca Creative Commons, ki daje uporabnikom največ možnosti za nadaljnjo uporabo dela, pri čemer morajo navesti avtorja.

Projekti

Financer:ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:P4-0053
Naslov:Endokrini, imunski in encimski odzivi pri zdravih in bolnih živalih

Financer:ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:P1-0207
Naslov:Toksini in biomembrane

Financer:ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:P1-0175
Naslov:Napredna anorganska kemija

Financer:ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Program financ.:Young researchers

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