New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease

Alzheimer's disease (AD) is a progressive neurodegenerative brain disease. Thus, drugs including donepezil, rivastigmine, and galantamine are not entirely effective in the treatment of this multifactorial disease. The present study evaluates eight derivatives (3a-3h) as candidates with stronger...

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Authors: Czarnecka, Kamila, Malgorzata, Girek, Krecisz, Pawel, Skibinski, Robert, Latka, Kamil, Jonczyk, Jakub, Bajda, Marek, Szymczyk, Piotr, Galita, Grzegorz, Kabzinski, Jacek, Majesterek, Ireneusz, Espargaró Colomé, Alba, Sabaté Lagunas, Raimon, Szymanski, Pawel
Format: article
Status:Published version
Publication Date:2023
Country:España
Institution:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repository:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/194019
Online Access:https://hdl.handle.net/2445/194019
Access Level:Open access
Keyword:Malaltia d'Alzheimer
Química farmacèutica
Alzheimer's disease
Pharmaceutical chemistry
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spelling New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's diseaseCzarnecka, KamilaMalgorzata, GirekKrecisz, PawelSkibinski, RobertLatka, KamilJonczyk, JakubBajda, MarekSzymczyk, PiotrGalita, GrzegorzKabzinski, JacekMajesterek, IreneuszEspargaró Colomé, AlbaSabaté Lagunas, RaimonSzymanski, PawelMalaltia d'AlzheimerQuímica farmacèuticaAlzheimer's diseasePharmaceutical chemistryAlzheimer's disease (AD) is a progressive neurodegenerative brain disease. Thus, drugs including donepezil, rivastigmine, and galantamine are not entirely effective in the treatment of this multifactorial disease. The present study evaluates eight derivatives (3a-3h) as candidates with stronger anti-AD potential but with less side effects. Reactive oxygen species (ROS) assays were used to assess oxidative stress which involve in the neurodegeneration. The neuroprotective properties of 3e against oxidative stress were done in three experiments using MTT test. The anti-AD potential was determined based on their anticholinesterase inhibition ability, determined using Ellman's method, Aβ aggregation potential according to thioflavin (Th) fluorescence assay, and their antioxidative and anti-inflammatory activities. Compound 3e exhibited moderate cholinesterase inhibition activity (AChE, IC50 = 0.131 µM; BuChE, IC50 = 0.116 µM; SI = 1.13), significant inhibition of Aβ(1-42) aggregation (55.7%, at 5 µM) and acceptable neuroprotective activity. Extensive analysis of in vitro and in vivo assays indicates that new cyclopentaquinoline derivatives offer promise as candidates for new anti-AD drugs.Taylor and Francis2023202320232023info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfapplication/pdfhttps://hdl.handle.net/2445/194019Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)reponame:Recercat. Dipósit de la Recerca de Catalunyainstname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)InglésReproducció del document publicat a: https://doi.org/10.1080/14756366.2022.2158822Journal of Enzyme Inhibition and Medicinal Chemistry, 2023, vol. 38, num. 1https://doi.org/10.1080/14756366.2022.2158822cc-by (c) Czarnecka, Kamila et al., 2023https://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccessoai:recercat.cat:2445/1940192026-05-29T05:05:01Z
dc.title.none.fl_str_mv New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
title New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
spellingShingle New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
Czarnecka, Kamila
Malaltia d'Alzheimer
Química farmacèutica
Alzheimer's disease
Pharmaceutical chemistry
title_short New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
title_full New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
title_fullStr New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
title_full_unstemmed New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
title_sort New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer's disease
dc.creator.none.fl_str_mv Czarnecka, Kamila
Malgorzata, Girek
Krecisz, Pawel
Skibinski, Robert
Latka, Kamil
Jonczyk, Jakub
Bajda, Marek
Szymczyk, Piotr
Galita, Grzegorz
Kabzinski, Jacek
Majesterek, Ireneusz
Espargaró Colomé, Alba
Sabaté Lagunas, Raimon
Szymanski, Pawel
author Czarnecka, Kamila
author_facet Czarnecka, Kamila
Malgorzata, Girek
Krecisz, Pawel
Skibinski, Robert
Latka, Kamil
Jonczyk, Jakub
Bajda, Marek
Szymczyk, Piotr
Galita, Grzegorz
Kabzinski, Jacek
Majesterek, Ireneusz
Espargaró Colomé, Alba
Sabaté Lagunas, Raimon
Szymanski, Pawel
author_role author
author2 Malgorzata, Girek
Krecisz, Pawel
Skibinski, Robert
Latka, Kamil
Jonczyk, Jakub
Bajda, Marek
Szymczyk, Piotr
Galita, Grzegorz
Kabzinski, Jacek
Majesterek, Ireneusz
Espargaró Colomé, Alba
Sabaté Lagunas, Raimon
Szymanski, Pawel
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Malaltia d'Alzheimer
Química farmacèutica
Alzheimer's disease
Pharmaceutical chemistry
topic Malaltia d'Alzheimer
Química farmacèutica
Alzheimer's disease
Pharmaceutical chemistry
description Alzheimer's disease (AD) is a progressive neurodegenerative brain disease. Thus, drugs including donepezil, rivastigmine, and galantamine are not entirely effective in the treatment of this multifactorial disease. The present study evaluates eight derivatives (3a-3h) as candidates with stronger anti-AD potential but with less side effects. Reactive oxygen species (ROS) assays were used to assess oxidative stress which involve in the neurodegeneration. The neuroprotective properties of 3e against oxidative stress were done in three experiments using MTT test. The anti-AD potential was determined based on their anticholinesterase inhibition ability, determined using Ellman's method, Aβ aggregation potential according to thioflavin (Th) fluorescence assay, and their antioxidative and anti-inflammatory activities. Compound 3e exhibited moderate cholinesterase inhibition activity (AChE, IC50 = 0.131 µM; BuChE, IC50 = 0.116 µM; SI = 1.13), significant inhibition of Aβ(1-42) aggregation (55.7%, at 5 µM) and acceptable neuroprotective activity. Extensive analysis of in vitro and in vivo assays indicates that new cyclopentaquinoline derivatives offer promise as candidates for new anti-AD drugs.
publishDate 2023
dc.date.none.fl_str_mv 2023
2023
2023
2023
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/194019
url https://hdl.handle.net/2445/194019
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Reproducció del document publicat a: https://doi.org/10.1080/14756366.2022.2158822
Journal of Enzyme Inhibition and Medicinal Chemistry, 2023, vol. 38, num. 1
https://doi.org/10.1080/14756366.2022.2158822
dc.rights.none.fl_str_mv cc-by (c) Czarnecka, Kamila et al., 2023
https://creativecommons.org/licenses/by/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc-by (c) Czarnecka, Kamila et al., 2023
https://creativecommons.org/licenses/by/4.0/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Taylor and Francis
publisher.none.fl_str_mv Taylor and Francis
dc.source.none.fl_str_mv Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
reponame:Recercat. Dipósit de la Recerca de Catalunya
instname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
instname_str Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
reponame_str Recercat. Dipósit de la Recerca de Catalunya
collection Recercat. Dipósit de la Recerca de Catalunya
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,812429

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