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DC Field | Value | Language |
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dc.contributor.author | Copmans, Danielle | - |
dc.contributor.author | Orellana Paucar, Adriana Monserrath | - |
dc.contributor.author | Steurs, Gert | - |
dc.contributor.author | Zhang, Yifan | - |
dc.contributor.author | Ny, Annelii | - |
dc.contributor.author | Foubert, Kenn | - |
dc.contributor.author | Exarchou, Vasiliki | - |
dc.contributor.author | Siekierska, Aleksandra | - |
dc.contributor.author | Kim, Youngju | - |
dc.contributor.author | De borggraeve, Wim | - |
dc.contributor.author | Dehaen, Wim | - |
dc.contributor.author | Pieters, Luc | - |
dc.contributor.author | De Witte, Peter AM | - |
dc.date.accessioned | 2018-06-21T15:10:11Z | - |
dc.date.available | 2018-06-21T15:10:11Z | - |
dc.date.issued | 2018 | - |
dc.identifier.issn | 0197-0186 | - |
dc.identifier.uri | https://www.sciencedirect.com/science/article/abs/pii/S0197018617302243 | - |
dc.description.abstract | Epilepsy is a neurological disease that affects more than 70 million people worldwide and is characterized by the presence of spontaneous unprovoked recurrent seizures. Existing anti-seizure drugs (ASDs) have side effects and fail to control seizures in 30% of patients due to drug resistance. Hence, safer and more efficacious drugs are sorely needed. Flavonoids are polyphenolic structures naturally present in most plants and consumed daily with no adverse effects reported. These structures have shown activity in several seizure and epilepsy animal models through allosteric modulation of GABAA receptors, but also via potent anti-inflammatory action in the brain. As such, dietary flavonoids offer an interesting source for ASD and anti-epileptogenic drug (AED) discovery, but their pharmaceutical potential is often hampered by metabolic instability and low oral bioavailability. It has been argued that their drug-likeness can be improved via methylation of the free hydroxyl groups, thereby dramatically enhancing metabolic stability and membrane transport, facilitating absorption and highly increasing bioavailability. Since no scientific data is available regarding the use of methylated flavonoids in the fight against epilepsy, we studied naringenin (NRG), kaempferol (KFL), and three methylated derivatives, i.e., naringenin 7-O-methyl ether (NRG-M), naringenin 40,7-dimethyl ether (NRG-DM), and kaempferide (40-O-methyl kaempferol) (KFD) in the zebrafish pentylenetetrazole (PTZ) seizure model. We demonstrate that the methylated flavanones NRG-DM and NRG-M are highly effective against PTZ-induced seizures in larval zebrafish, whereas NRG and the flavonols KFL and KFD possess only a limited activity. Moreover, we show that NRG-DM is active in two standard acute mouse seizure models, i.e., the timed i.v. PTZ seizure model and the 6-Hz psychomotor seizure model. Based on these results, NRG-DM is proposed as a lead compound that is worth further investigation for the treatment of generalized seizures and drug-resistant focal seizures. Our data therefore highlights the potential of methylated flavonoids in the search for new and improved ASDs. | - |
dc.language.iso | es_ES | - |
dc.source | Neurochemistry International | - |
dc.subject | EPILEPSY | - |
dc.subject | DRUG DISCOVERY | - |
dc.subject | METHYLATED FLAVONOIDS | - |
dc.subject | NARINGENIN | - |
dc.subject | ZEBRAFISH | - |
dc.subject | MOUSE | - |
dc.title | Methylated flavonoids as antiseizure agents: Naringenin 4′,7-dimethyl ether attenuates epileptic seizures in zebrafish and mouse models | - |
dc.title.alternative | null | - |
dc.type | ARTÍCULO | - |
dc.ucuenca.idautor | 0000-0002-9804-8410 | - |
dc.ucuenca.idautor | 0103903142 | - |
dc.ucuenca.idautor | 0000-0002-9779-7743 | - |
dc.ucuenca.idautor | 0000-0003-0916-1073 | - |
dc.ucuenca.idautor | 6603211543 | - |
dc.ucuenca.idautor | 24468130500 | - |
dc.ucuenca.idautor | 6507452458 | - |
dc.ucuenca.idautor | 000-0003-4907-605X | - |
dc.ucuenca.idautor | 55699547000 | - |
dc.ucuenca.idautor | 0000-0001-7813-6192 | - |
dc.ucuenca.idautor | 0000-0002-9597-0629 | - |
dc.ucuenca.idautor | 7006602213 | - |
dc.ucuenca.idautor | 0000-0002-9989-9567 | - |
dc.identifier.doi | 10.1016/j.neuint.2017.11.011 | - |
dc.ucuenca.embargoend | 2050-12-31 | - |
dc.ucuenca.version | Versión publicada | - |
dc.ucuenca.embargointerno | 2050-12-31 | - |
dc.ucuenca.areaconocimientounescoamplio | 09 - Salud y Bienestar | - |
dc.ucuenca.afiliacion | Copmans, D., KU Leuven (Katholieke Universiteit Leuven), Leuven, Belgica | - |
dc.ucuenca.afiliacion | Orellana, A., Universidad de Cuenca, Facultad de Ciencias Químicas, Cuenca, Ecuador | - |
dc.ucuenca.afiliacion | Steurs, G., KU Leuven (Katholieke Universiteit Leuven), Leuven, Belgica | - |
dc.ucuenca.afiliacion | Zhang, Y., KU Leuven (Katholieke Universiteit Leuven), Leuven, Belgica | - |
dc.ucuenca.afiliacion | Ny, A., KU Leuven (Katholieke Universiteit Leuven), Leuven, Belgica | - |
dc.ucuenca.afiliacion | Foubert, K., Universidad de Amberes (University of Antwerp), Amberes, Belgica | - |
dc.ucuenca.afiliacion | Exarchou, V., Universidad de Amberes (University of Antwerp), Amberes, Belgica | - |
dc.ucuenca.afiliacion | Siekierska, A., KU Leuven (Katholieke Universiteit Leuven), Leuven, Belgica | - |
dc.ucuenca.afiliacion | Kim, Y., KU Leuven (Katholieke Universiteit Leuven), Leuven, Belgica | - |
dc.ucuenca.afiliacion | De borggraeve, W., KU Leuven (Katholieke Universiteit Leuven), Leuven, Belgica | - |
dc.ucuenca.afiliacion | Dehaen, W., KU Leuven (Katholieke Universiteit Leuven), Leuven, Belgica | - |
dc.ucuenca.afiliacion | Pieters, L., Universidad de Amberes (University of Antwerp), Amberes, Belgica | - |
dc.ucuenca.afiliacion | De Witte, P., KU Leuven (Katholieke Universiteit Leuven), Leuven, Belgica | - |
dc.ucuenca.correspondencia | De Witte, Peter AM, peter.dewitte@kuleuven.be | - |
dc.ucuenca.volumen | Vol. 112 | - |
dc.ucuenca.indicebibliografico | SCOPUS | - |
dc.ucuenca.factorimpacto | 1.241 | - |
dc.ucuenca.cuartil | Q2 | - |
dc.ucuenca.numerocitaciones | 0 | - |
dc.ucuenca.areaconocimientofrascatiamplio | 3. Ciencias Médicas y de la Salud | - |
dc.ucuenca.areaconocimientofrascatiespecifico | 3.1 Medicina Básica | - |
dc.ucuenca.areaconocimientofrascatidetallado | 3.1.5 Farmacología y Farmacia | - |
dc.ucuenca.areaconocimientounescoespecifico | 091 - Salud | - |
dc.ucuenca.areaconocimientounescodetallado | 0916 - Farmacia | - |
dc.ucuenca.urifuente | https://www.journals.elsevier.com/neurochemistry-international | - |
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