Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Brazilian Journal of Pharmaceutical Sciences |
Texto Completo: | https://www.revistas.usp.br/bjps/article/view/181445 |
Resumo: | The effects of new derivatives of caffeine-8-thioglycolic acid (100 μM) on isolated rat brain synaptosomes, human neuroblastoma cell line SH-SY5Y and human recombinant MAOB enzyme (hMAOB) (1 μM) were evaluated. Most of the compounds, administered alone, didn’t show statistically significant neurotoxic effects on SH-SY5Y, when compared to the control (non-treated cells). Of all studied structures JTA-2Ox, JTA-11, JTA-12 and JTA-13 decreased cell viability. In combination with 6-hydroxydopamine (6-OHDA) (100 μM), only JTA-1 and JTA-2 revealed neuroprotective effects, stronger than those of caffeine. All compounds administered alone revealed, neurotoxic effects on synaptosomes, as compared to nontreated synaptosomes. JTA-1, JTA-2 and JTA-3 showed lowest neurotoxic effects and were investigated in a model of 6-OHDA-induced oxidative stress. In this model of neurotoxicity, only JTA-1 and JTA-2 showed statistically significant neuroprotective effect, by preserving the synaptosomal viability and the level of reduced glutathione. Inhibition of hMAOB, was revealed by JTA-1 and JTA-2. They inhibited the enzyme by 23% and 25% respectively, thus approaching the selegiline activity, which was 42%. The possible mechanisms of neuroprotection of JTA-1 and JTA-2 might be a result from the inhibition of hMAOB, which catalyze the production of neurotoxic p-quinone from 6-OHDA. |
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Brazilian Journal of Pharmaceutical Sciences |
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Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amidesNeuroprotectionCaffeineSynaptosomesSH-SY5YhMAOBThe effects of new derivatives of caffeine-8-thioglycolic acid (100 μM) on isolated rat brain synaptosomes, human neuroblastoma cell line SH-SY5Y and human recombinant MAOB enzyme (hMAOB) (1 μM) were evaluated. Most of the compounds, administered alone, didn’t show statistically significant neurotoxic effects on SH-SY5Y, when compared to the control (non-treated cells). Of all studied structures JTA-2Ox, JTA-11, JTA-12 and JTA-13 decreased cell viability. In combination with 6-hydroxydopamine (6-OHDA) (100 μM), only JTA-1 and JTA-2 revealed neuroprotective effects, stronger than those of caffeine. All compounds administered alone revealed, neurotoxic effects on synaptosomes, as compared to nontreated synaptosomes. JTA-1, JTA-2 and JTA-3 showed lowest neurotoxic effects and were investigated in a model of 6-OHDA-induced oxidative stress. In this model of neurotoxicity, only JTA-1 and JTA-2 showed statistically significant neuroprotective effect, by preserving the synaptosomal viability and the level of reduced glutathione. Inhibition of hMAOB, was revealed by JTA-1 and JTA-2. They inhibited the enzyme by 23% and 25% respectively, thus approaching the selegiline activity, which was 42%. The possible mechanisms of neuroprotection of JTA-1 and JTA-2 might be a result from the inhibition of hMAOB, which catalyze the production of neurotoxic p-quinone from 6-OHDA.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2020-12-09info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/18144510.1590/s2175-97902019000318255Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18255 Brazilian Journal of Pharmaceutical Sciences; v. 56 (2020); e18255 Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18255 2175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/181445/168389Copyright (c) 2020 Brazilian Journal of Pharmaceutical Scienceshttp://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessKasabova-Angelova, Alexandra Kondeva-Burdina, Magdalena Mitkov, Javor Georgieva, Maya Tzankova, Virginia Zlatkov, Alexander 2021-06-12T19:46:54Zoai:revistas.usp.br:article/181445Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2021-06-12T19:46:54Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false |
dc.title.none.fl_str_mv |
Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides |
title |
Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides |
spellingShingle |
Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides Kasabova-Angelova, Alexandra Neuroprotection Caffeine Synaptosomes SH-SY5Y hMAOB |
title_short |
Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides |
title_full |
Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides |
title_fullStr |
Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides |
title_full_unstemmed |
Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides |
title_sort |
Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides |
author |
Kasabova-Angelova, Alexandra |
author_facet |
Kasabova-Angelova, Alexandra Kondeva-Burdina, Magdalena Mitkov, Javor Georgieva, Maya Tzankova, Virginia Zlatkov, Alexander |
author_role |
author |
author2 |
Kondeva-Burdina, Magdalena Mitkov, Javor Georgieva, Maya Tzankova, Virginia Zlatkov, Alexander |
author2_role |
author author author author author |
dc.contributor.author.fl_str_mv |
Kasabova-Angelova, Alexandra Kondeva-Burdina, Magdalena Mitkov, Javor Georgieva, Maya Tzankova, Virginia Zlatkov, Alexander |
dc.subject.por.fl_str_mv |
Neuroprotection Caffeine Synaptosomes SH-SY5Y hMAOB |
topic |
Neuroprotection Caffeine Synaptosomes SH-SY5Y hMAOB |
description |
The effects of new derivatives of caffeine-8-thioglycolic acid (100 μM) on isolated rat brain synaptosomes, human neuroblastoma cell line SH-SY5Y and human recombinant MAOB enzyme (hMAOB) (1 μM) were evaluated. Most of the compounds, administered alone, didn’t show statistically significant neurotoxic effects on SH-SY5Y, when compared to the control (non-treated cells). Of all studied structures JTA-2Ox, JTA-11, JTA-12 and JTA-13 decreased cell viability. In combination with 6-hydroxydopamine (6-OHDA) (100 μM), only JTA-1 and JTA-2 revealed neuroprotective effects, stronger than those of caffeine. All compounds administered alone revealed, neurotoxic effects on synaptosomes, as compared to nontreated synaptosomes. JTA-1, JTA-2 and JTA-3 showed lowest neurotoxic effects and were investigated in a model of 6-OHDA-induced oxidative stress. In this model of neurotoxicity, only JTA-1 and JTA-2 showed statistically significant neuroprotective effect, by preserving the synaptosomal viability and the level of reduced glutathione. Inhibition of hMAOB, was revealed by JTA-1 and JTA-2. They inhibited the enzyme by 23% and 25% respectively, thus approaching the selegiline activity, which was 42%. The possible mechanisms of neuroprotection of JTA-1 and JTA-2 might be a result from the inhibition of hMAOB, which catalyze the production of neurotoxic p-quinone from 6-OHDA. |
publishDate |
2020 |
dc.date.none.fl_str_mv |
2020-12-09 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/181445 10.1590/s2175-97902019000318255 |
url |
https://www.revistas.usp.br/bjps/article/view/181445 |
identifier_str_mv |
10.1590/s2175-97902019000318255 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/181445/168389 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2020 Brazilian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/4.0 info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2020 Brazilian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/4.0 |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
dc.source.none.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18255 Brazilian Journal of Pharmaceutical Sciences; v. 56 (2020); e18255 Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18255 2175-9790 1984-8250 reponame:Brazilian Journal of Pharmaceutical Sciences instname:Universidade de São Paulo (USP) instacron:USP |
instname_str |
Universidade de São Paulo (USP) |
instacron_str |
USP |
institution |
USP |
reponame_str |
Brazilian Journal of Pharmaceutical Sciences |
collection |
Brazilian Journal of Pharmaceutical Sciences |
repository.name.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP) |
repository.mail.fl_str_mv |
bjps@usp.br||elizabeth.igne@gmail.com |
_version_ |
1787713372380200960 |