English   español  
Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/171540
Share/Impact:
Statistics
logo share SHARE logo core CORE   Add this article to your Mendeley library MendeleyBASE

Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL
Exportar a otros formatos:

Title

Evaluation of the bioavailability and metabolism of nitroderivatives of hydroxytyrosol Using Caco-2 and HepG2 human cell models

AuthorsGallardo, Elena; Sarriá, Beatriz ; Espartero, José L.; González Correa, José A.; Bravo, Laura ; Mateos, Raquel
KeywordsParkinson’s disease
Metabolism
Nitrocatechols
Hydroxytyrosol
Bioavailability
Issue Date2016
PublisherAmerican Chemical Society
CitationJournal of Agricultural and Food Chemistry 64(11): 2289-2297 (2016)
AbstractConsidering that nitrocatechols present putative effects against Parkinson's disease, the absorption and metabolism of nitroderivatives of hydroxytyrosol (HT) were assessed using human cell model systems. The test compounds nitrohydroxytyrosol (NOHT), nitrohydroxytyrosyl acetate (NOHT-A), and ethyl nitrohydroxytyrosyl ether (NOHT-E) were efficiently transferred across human Caco-2 cell monolayers as an intestinal barrier model, NOHT-A and NOHT-E being better (p < 0.05) absorbed (absorption rate (AR) = 1.4 ± 0.1 and 1.5 ± 0.2, respectively) than their precursor, NOHT (AR = 1.1 ± 0.1). A significant amount of the absorbed compounds remained unconjugated (81, 70, and 33% for NOHT, NOHT-A, and NOHT-E, respectively) after incubation in Caco-2 cells, being available for hepatic metabolism. Nitrocatechols were extensively taken up and metabolized by human hepatoma HepG2 cells as a model of the human liver. Both studies revealed extensive hydrolysis of NOHT-A into NOHT, whereas NOHT-E was not hydrolyzed. Glucuronide (75-55%), methylglucuronide (25-33%), and methyl derivatives (0-12%) were the main nitrocatechol metabolites detected after metabolism in Caco-2 and HepG2 cells. In conclusion, NOHT, NOHT-A, and NOHT-E show high in vitro bioavailability and are extensively metabolized by hepatic cells.
Publisher version (URL)https://doi.org/10.1021/acs.jafc.6b00401
URIhttp://hdl.handle.net/10261/171540
Identifiersdoi: 10.1021/acs.jafc.6b00401
e-issn: 1520-5118
issn: 0021-8561
Appears in Collections:(ICTAN) Artículos
Files in This Item:
File Description SizeFormat 
evaluatG2.pdf826,12 kBAdobe PDFThumbnail
View/Open
Show full item record
Review this work
 

Related articles:


WARNING: Items in Digital.CSIC are protected by copyright, with all rights reserved, unless otherwise indicated.