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Evaluation of the Bioavailability and Metabolism of Nitroderivatives of Hydroxytyrosol Using Caco-2 and HepG2 Human Cell Models.
Gallardo, Elena; Sarria, Beatriz; Espartero, José Luis; Gonzalez Correa, José Antonio; Bravo-Clemente, Laura; Mateos, Raquel.
Afiliação
  • Gallardo E; Department of Metabolism and Nutrition, Institute of Food Science, Technology and Nutrition (ICTAN), CSIC , Madrid, Spain.
  • Sarria B; Department of Organic and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Seville, Seville, Spain.
  • Espartero JL; Department of Pharmacology and Therapeutics, School of Medicine, University of Malaga , Malaga, Spain.
  • Gonzalez Correa JA; Department of Metabolism and Nutrition, Institute of Food Science, Technology and Nutrition (ICTAN), CSIC , Madrid, Spain.
  • Bravo-Clemente L; Department of Organic and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Seville, Seville, Spain.
  • Mateos R; Department of Pharmacology and Therapeutics, School of Medicine, University of Malaga , Malaga, Spain.
J Agric Food Chem ; 64(11): 2289-97, 2016 Mar 23.
Article em En | MEDLINE | ID: mdl-26915652
Considering 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 (NO2HT), nitrohydroxytyrosyl acetate (NO2HT-A), and ethyl nitrohydroxytyrosyl ether (NO2HT-E) were efficiently transferred across human Caco-2 cell monolayers as an intestinal barrier model, NO2HT-A and NO2HT-E being better (p < 0.05) absorbed (absorption rate (AR) = 1.4 ± 0.1 and 1.5 ± 0.2, respectively) than their precursor, NO2HT (AR = 1.1 ± 0.1). A significant amount of the absorbed compounds remained unconjugated (81, 70, and 33% for NO2HT, NO2HT-A, and NO2HT-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 NO2HT-A into NO2HT, whereas NO2HT-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, NO2HT, NO2HT-A, and NO2HT-E show high in vitro bioavailability and are extensively metabolized by hepatic cells.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Álcool Feniletílico / Mucosa Intestinal / Fígado / Nitrocompostos Limite: Humans Idioma: En Revista: J Agric Food Chem Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Espanha País de publicação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Álcool Feniletílico / Mucosa Intestinal / Fígado / Nitrocompostos Limite: Humans Idioma: En Revista: J Agric Food Chem Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Espanha País de publicação: Estados Unidos