Electronic Resource
Evaluation of the bioavailability and metabolism of nitroderivatives of hydroxytyrosol Using Caco-2 and HepG2 human cell models
| العنوان: | Evaluation of the bioavailability and metabolism of nitroderivatives of hydroxytyrosol Using Caco-2 and HepG2 human cell models |
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| المؤلفون: | Junta de Andalucía, Gallardo, Elena, Sarriá, Beatriz, Espartero, José L., González Correa, José A., Bravo, Laura, Mateos, Raquel |
| بيانات النشر: | American Chemical Society 2016 |
| نوع الوثيقة: | Electronic Resource |
| مستخلص: | 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 (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. |
| مصطلحات الفهرس: | Parkinson’s disease, Metabolism, Nitrocatechols, Hydroxytyrosol, Bioavailability, artículo |
| URL: | Postprint Sí |
| الاتاحة: | Open access content. Open access content openAccess |
| ملاحظة: | English |
| Other Numbers: | CTK oai:digital.csic.es:10261/171540 Journal of Agricultural and Food Chemistry 64(11): 2289-2297 (2016) 10.1021/acs.jafc.6b00401 26915652 1138010844 |
| المصدر المساهم: | CSIC From OAIster®, provided by the OCLC Cooperative. |
| رقم الانضمام: | edsoai.on1138010844 |
| قاعدة البيانات: | OAIster |
| الوصف غير متاح. |