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dc.contributor.authorChlebek, Jakubes_ES
dc.contributor.authorDe Simone, Angelaes_ES
dc.contributor.authorHošťálková, Annaes_ES
dc.contributor.authorOpletal, Lubomíres_ES
dc.contributor.authorPérez, Concepciónes_ES
dc.contributor.authorPérez, Daniel I.es_ES
dc.contributor.authorHavlíková, Luciees_ES
dc.contributor.authorCahlíková, Luciees_ES
dc.contributor.authorAndrisano, Vincenzaes_ES
dc.identifier.citationFitoterapia 109: 241–247 ( 2016)es_ES
dc.description22 p.-2 fig.-3 tab.es_ES
dc.description.abstractIn our ongoing study focused on Corydalis cava (Fumariaceae), used in folk medicine in the treatment of memory dysfunctions, we have investigated fifteen previously isolated alkaloids for their potential multifunctional activity on Alzheimer's disease (AD) targets. Determination of ß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibition was carried out using a BACE1-Immobilized Enzyme Reactor (IMER) by validating the assay with a multi-well plate format Fluorescence Resonance Energy Transfer (FRET) assay. Seven alkaloids out of fifteen were found to be active, with (−)-corycavamine (3) and (+)-corynoline (5) demonstrating the highest BACE1 inhibition activity, in the micromolar range, in a concentration dependent manner. BACE1-IMER was found to be a valid device for the fast screening of inhibitors and the determination of their potency. In a permeation assay (PAMPA) for the prediction of blood–brain barrier (BBB) penetration, the most active compounds, (−)-corycavamine (3) and (+)-corynoline (5), were found to be able to cross the BBB. Not all compounds showed activity against glycogen synthase kinase-3β (GSK-3β) and casein kinase-1δ (CK-1δ). On the basis of the reported results, we found that some C. cava alkaloids have multifunctional activity against AD targets (prolyl oligopeptidase, cholinesterases and BACE1). Moreover, we tried to elucidate the treatment effectivity (rational use) of its extract in memory dysfunction in folk medicine.es_ES
dc.description.sponsorshipThis project was supported by grant SVV UK 260 063, Charles University grant No. 17/2012/UNCE. The publication was also co-financed by the European Social Fund and by the state budget of the Czech Republic, project No. CZ.1.07/2.3.00/20.0235, the title of the project: TEAB and UniRimini.es_ES
dc.subjectBACE1 inhibitorses_ES
dc.subjectImmobilized enzyme reactores_ES
dc.subjectCorydalis cava alkaloidses_ES
dc.subjectPAMPA assayes_ES
dc.titleApplication of BACE1 immobilized enzyme reactor for the characterization of multifunctional alkaloids from Corydalis cava (Fumariaceae) as Alzheimer's disease targetses_ES
dc.description.peerreviewedPeer reviewedes_ES
dc.relation.publisherversionhttp://dx.doi.org/ 10.1016/j.fitote.2016.01.008es_ES
dc.contributor.funderCharles University (Czech Republic)es_ES
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