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Pharmacokinetic characterization of carnosol from rosemary (Salvia Rosmarinus) in male C57BL/6 mice and inhibition profile in human cytochrome P450 enzymes.
- Source :
-
Toxicology and applied pharmacology [Toxicol Appl Pharmacol] 2021 Nov 15; Vol. 431, pp. 115729. Date of Electronic Publication: 2021 Sep 27. - Publication Year :
- 2021
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Abstract
- 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.<br /> (Copyright © 2021. Published by Elsevier Inc.)
- Subjects :
- Abietanes administration & dosage
Abietanes blood
Abietanes isolation & purification
Administration, Oral
Animals
Biological Availability
Cottonseed Oil chemistry
Cytochrome P-450 Enzyme Inhibitors administration & dosage
Cytochrome P-450 Enzyme Inhibitors blood
Cytochrome P-450 Enzyme Inhibitors isolation & purification
Drug Stability
Food Preservatives administration & dosage
Food Preservatives isolation & purification
HT29 Cells
Hep G2 Cells
Humans
Isoenzymes
Male
Membrane Transport Proteins drug effects
Membrane Transport Proteins metabolism
Mice, Inbred C57BL
Rosmarinus chemistry
Temperature
Mice
Abietanes pharmacokinetics
Cytochrome P-450 Enzyme Inhibitors pharmacokinetics
Cytochrome P-450 Enzyme System metabolism
Food Preservatives pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1096-0333
- Volume :
- 431
- Database :
- MEDLINE
- Journal :
- Toxicology and applied pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 34592323
- Full Text :
- https://doi.org/10.1016/j.taap.2021.115729