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Toxicol Appl Pharmacol ; 431: 115729, 2021 11 15.
Artículo en Inglés | MEDLINE | ID: mdl-34592323

RESUMEN

Rosemary (Salvia Rosmarinus) is a rich source of dietary diterpenes with carnosol as one of the major polyphenols used to standardize rosemary extracts approved as a food preservative, however, at present there is not any information on the murine pharmacokinetic profile of carnosol or its potential for drug interactions. The present study utilizes cell-free, cell-based, and animal-based experiments to define the pharmacokinetic profile of the food based phytochemical carnosol. Mice were administered carnosol (100 mg/kg body weight) by oral gavage and plasma levels were analyzed by LC-MS/MS to establish a detailed pharmacokinetic profile. The maximum plasma concentration exceeded 1 µM after a single administration. The results are significant as they offer insights on the potential for food-drug interactions between carnosol from rosemary and active pharmaceutical ingredients. Carnosol was observed to inhibit selected CYP450 enzymes and modulate metabolic enzymes and transporters in in vitro assays.


Asunto(s)
Abietanos/farmacocinética , Inhibidores Enzimáticos del Citocromo P-450/farmacocinética , Sistema Enzimático del Citocromo P-450/metabolismo , Conservantes de Alimentos/farmacocinética , Abietanos/administración & dosificación , Abietanos/sangre , Abietanos/aislamiento & purificación , Administración Oral , Animales , Disponibilidad Biológica , Aceite de Semillas de Algodón/química , Inhibidores Enzimáticos del Citocromo P-450/administración & dosificación , Inhibidores Enzimáticos del Citocromo P-450/sangre , Inhibidores Enzimáticos del Citocromo P-450/aislamiento & purificación , Estabilidad de Medicamentos , Conservantes de Alimentos/administración & dosificación , Conservantes de Alimentos/aislamiento & purificación , Células HT29 , Células Hep G2 , Humanos , Isoenzimas , Masculino , Proteínas de Transporte de Membrana/efectos de los fármacos , Proteínas de Transporte de Membrana/metabolismo , Ratones Endogámicos C57BL , Rosmarinus/química , Temperatura
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