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New insights into the effects of organometallic ruthenium complexes on nicotinic acetylcholine receptors
ID
Trobec, Tomaž
(
Author
),
ID
Lamassiaude, Nicolas
(
Author
),
ID
Benoit, Evelyne
(
Author
),
ID
Žužek, Monika C.
(
Author
),
ID
Sepčić, Kristina
(
Author
),
ID
Kladnik, Jerneja
(
Author
),
ID
Turel, Iztok
(
Author
),
ID
Aráoz, Rómulo
(
Author
),
ID
Frangež, Robert
(
Author
)
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https://www.sciencedirect.com/science/article/pii/S0009279724003594
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Abstract
Nicotinic acetylcholine receptors (nAChRs) are expressed in excitable and non-excitable cells of the organism. Extensive studies suggest that nAChR ligands have therapeutic potential, notably for neurological and psychiatric disorders. Organometallic ruthenium complexes are known to inhibit several medically important enzymes such as cholinesterases. In addition, they can also interact with muscle- and neuronal-subtype nAChRs. The present study aimed to investigate the direct effects of three organometallic ruthenium complexes, [(η$^6$-p-cymene)Ru(II)(5-nitro-1,10-phenanthroline)Cl]Cl (C1–Cl), [(η$^6$-p-cymene)Ru(II)(1-hydroxypyridine-2(1H)-thionato)Cl] (C1a) and [(η$^6$-p-cymene)Ru(II)(1-hydroxy-3-methoxypyridine-2(1H)-thionato)pta]PF$_6$ (C1), on muscle-subtype (Torpedo) nAChRs and on the two most abundant human neuronal-subtype nAChRs in the CNS (α4β2 and α7) expressed in Xenopus laevis oocytes, using the two-electrode voltage-clamp. The results show that none of the three compounds had agonistic activity on any of the nAChR subtypes studied. In contrast, C1–Cl reversibly blocked Torpedo nAChR (half-reduction of ACh-evoked peak current amplitude by 332 nM of compound). When tested at 10 μM, C1–Cl was statistically more potent to inhibit TorpedonAChR than α4β2 and α7 nAChRs. Similar results of C1 effects were obtained on Torpedo and α4β2 nAChRs, while no action of the compound was detected on α7 nAChRs. Finally, the effects of C1a were statistically similar on the three nAChR subtypes but, in contrast to C1–Cl and C1, the inhibition was hardly reversible. These results, together with our previous studies on isolated mouse neuromuscular preparations, strongly suggest that C1–Cl is, among the three compounds studied, the only molecule that could be used as a potential myorelaxant drug.
Language:
English
Keywords:
organometallic ruthenium complexes
,
nicotinic acetylcholine receptors
,
nicotinic antagonists
,
electrophysiology
,
two-electrode voltage-clamp technique
Work type:
Article
Typology:
1.01 - Original Scientific Article
Organization:
VF - Veterinary Faculty
BF - Biotechnical Faculty
FKKT - Faculty of Chemistry and Chemical Technology
Publication status:
Published
Publication version:
Version of Record
Year:
2024
Number of pages:
7 str.
Numbering:
Vol. 402, art. 111213
PID:
20.500.12556/RUL-160689
UDC:
616-092
ISSN on article:
1872-7786
DOI:
10.1016/j.cbi.2024.111213
COBISS.SI-ID:
205689347
Publication date in RUL:
03.09.2024
Views:
83
Downloads:
48
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Record is a part of a journal
Title:
Chemico-biological interactions
Publisher:
Elsevier
ISSN:
1872-7786
COBISS.SI-ID:
23211013
Licences
License:
CC BY 4.0, Creative Commons Attribution 4.0 International
Link:
http://creativecommons.org/licenses/by/4.0/
Description:
This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.
Projects
Funder:
ARIS - Slovenian Research and Innovation Agency
Project number:
P4-0053
Name:
Endokrini, imunski in encimski odzivi pri zdravih in bolnih živalih
Funder:
ARIS - Slovenian Research and Innovation Agency
Project number:
P1-0207
Name:
Toksini in biomembrane
Funder:
ARIS - Slovenian Research and Innovation Agency
Project number:
P1-0175
Name:
Napredna anorganska kemija
Funder:
ARIS - Slovenian Research and Innovation Agency
Project number:
BI-FR/21-22-PROTEUS-002
Acronym:
PROTEUS
Funder:
ARIS - Slovenian Research and Innovation Agency
Funding programme:
Young researchers
Funder:
Other - Other funder or multiple funders
Funding programme:
French Alternative Energies and Atomic Energy Commission (CEA)
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