Abstract | BACKGROUND:
Quercetin (Q) is one of the most abundant flavonoids in human dietary sources and has been related to the capacity to ameliorate obesity-related pathologies. Quercetin-3-O-β-d-glucuronide (Q3GA) is supposed to be the main metabolite in blood circulation, but the intracellular final effectors for its activity are still unknown. HYPOTHESIS/PURPOSE: To identify and quantitate the intracellular metabolites in hypertrophied adipocytes incubated with Q or Q3GA and to correlate them with the intracellular generation of oxygen radical species (ROS). METHODS: Cytoplasmic fractions were obtained and quercetin metabolites were determined by liquid chromatography coupled to a time-of-flight mass detector with electrospray ionization (HPLC-DAD-ESI-TOF). Intracellular ROS generation was measured by a ROS-sensitive fluorescent probe. RESULTS: Both Q and Q3GA were absorbed by hypertrophied adipocytes and metabolized to some extent to Q3GA and Q, respectively, but Q absorption was more efficient (1.92 ± 0.03µg/µg protein) and faster than that of Q3GA (0.12 ± 0.0015µg/µg protein), leading to a higher intracellular concentration of the aglycone. Intracellular decrease of ROS correlated with the presence of the most abundant quercetin metabolite. CONCLUSION: Q and Q3GA are efficiently absorbed by hypertrophied adipocytes and metabolized to some extent to Q3GA and Q, respectively. The intracellular decrease of ROS in a hypertrophied adipocyte model treated with Q or Q3GA is correlated with the most abundant intracellular metabolite for the first time. Both compounds might be able to reach other intracellular targets, thus contributing to their bioactivity.
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Authors | María Herranz-López, Isabel Borrás-Linares, Mariló Olivares-Vicente, Julio Gálvez, Antonio Segura-Carretero, Vicente Micol |
Journal | Phytomedicine : international journal of phytotherapy and phytopharmacology
(Phytomedicine)
Vol. 25
Pg. 25-28
(Feb 15 2017)
ISSN: 1618-095X [Electronic] Germany |
PMID | 28190467
(Publication Type: Journal Article)
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Copyright | Copyright © 2016 Elsevier GmbH. All rights reserved. |
Chemical References |
- Glucuronides
- Plant Extracts
- Reactive Oxygen Species
- Quercetin
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Topics |
- 3T3-L1 Cells
- Adipocytes
(drug effects, metabolism)
- Adipose Tissue
(metabolism)
- Animals
- Chromatography, High Pressure Liquid
- Glucuronides
(metabolism)
- Hibiscus
(chemistry)
- Humans
- Hypertrophy
- Mice
- Obesity
(metabolism)
- Oxidative Stress
(drug effects)
- Phytotherapy
- Plant Extracts
(pharmacology, therapeutic use)
- Quercetin
(analogs & derivatives, metabolism, pharmacology, therapeutic use)
- Reactive Oxygen Species
(metabolism)
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