| Registro completo |
| Provedor de dados: |
BJPS
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| País: |
Brazil
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| Título: |
Neuroprotective and MAOB inhibitory effects of a series of caffeine-8-thioglycolic acid amides
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| Autores: |
Kasabova-Angelova,Alexandra
Kondeva-Burdina,Magdalena
Mitkov,Javor
Georgieva,Maya
Tzankova,Virginia
Zlatkov,Alexander
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| Data: |
2020-01-01
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| Ano: |
2020
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| Palavras-chave: |
Neuroprotection
Caffeine
Synaptosomes
SH-SY5Y
HMAOB
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| 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 non-treated 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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| Tipo: |
Info:eu-repo/semantics/article
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| Idioma: |
Inglês
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| Identificador: |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100529
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| Editor: |
Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
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| Relação: |
10.1590/s2175-97902019000318255
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| Formato: |
text/html
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| Fonte: |
Brazilian Journal of Pharmaceutical Sciences v.56 2020
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| Direitos: |
info:eu-repo/semantics/openAccess
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