| Journal: | Brazilian Journal of Pharmaceutical Sciences |
| Database: | PERIÓDICA |
| System number: | 000451435 |
| ISSN: | 1984-8250 |
| Authors: | Kasabova Angelova, Alexandra1 Kondeva Burdina, Magdalena1 Mitkov, Javor1 Georgieva, Maya1 Tzankova, Virginia1 Zlatkov, Alexander1 |
| Institutions: | 1Medical University of Sofia, Faculty of Pharmacy, Sofía. Bulgaria |
| Year: | 2020 |
| Volumen: | 56 |
| Country: | Brasil |
| Language: | Inglés |
| Document type: | Artículo |
| Approach: | Experimental, aplicado |
| English abstract | 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 |
| Disciplines: | Medicina, Química |
| Keyword: | Medicina experimental, Farmacología, Neuroprotección, Cafeína, Sinaptosomas |
| Keyword: | Experimental medicine, Pharmacology, Neuroprotection, Caffeine, Synaptosomes |
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