New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study
The intake of hesperidin-rich sources, mostly found in orange juice, can decrease cardiometabolic risk, potentially linked to the gut microbial phase-II hesperetin derivatives. However, the low hesperidin solubility hampers its bioavailability and microbial metabolism, yielding a high inter-individu...
| Autores: | , , , |
|---|---|
| Tipo de recurso: | artículo |
| Estado: | Versión publicada |
| Fecha de publicación: | 2021 |
| País: | España |
| Institución: | Consejo Superior de Investigaciones Científicas (CSIC) |
| Repositorio: | DIGITAL.CSIC. Repositorio Institucional del CSIC |
| OAI Identifier: | oai:digital.csic.es:10261/411930 |
| Acceso en línea: | http://hdl.handle.net/10261/411930 |
| Access Level: | acceso abierto |
| Palabra clave: | Flavanones Gut microbiota Citrus Orange Hesperidin Lemon Eriocitrin Pharmacokinetics Hesperetin metabolites Eriodictyol metabolites |
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New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic studyÁvila-Gálvez, María ÁngelesGiménez-Bastida, J. A.González-Sarrías, AntonioEspín de Gea, Juan CarlosFlavanonesGut microbiotaCitrusOrangeHesperidinLemonEriocitrinPharmacokineticsHesperetin metabolitesEriodictyol metabolitesThe intake of hesperidin-rich sources, mostly found in orange juice, can decrease cardiometabolic risk, potentially linked to the gut microbial phase-II hesperetin derivatives. However, the low hesperidin solubility hampers its bioavailability and microbial metabolism, yielding a high inter-individual variability (high vs. low-producers) that prevents consistent health-related evidence. Contrarily, the human metabolism of (lemon) eriocitrin is hardly known. We hypothesize that the higher solubility of (lemon) eriocitrin vs. (orange) hesperidin might yield more bioavailable metabolites than hesperidin. A randomized-crossover human pharmacokinetic study (n = 16) compared the bioavailability and metabolism of flavanones from lemon and orange extracts and postprandial changes in oxidative, inflammatory, and metabolic markers after a high-fat-high-sugars meal. A total of 17 phase-II flavanone-derived metabolites were identified. No significant biomarker changes were observed. Plasma and urinary concentrations of all metabolites, including hesperetin metabolites, were higher after lemon extract intake. Total plasma metabolites showed significantly mean lower Tmax (6.0 ± 0.4 vs. 8.0 ± 0.5 h) and higher Cmax and AUC values after lemon extract intake. We provide new insights on hesperetin-eriodictyol interconversion and naringenin formation from hesperidin in humans. Our results suggest that regular consumption of a soluble and eco-friendly eriocitrin-rich lemon extract could provide a circulating concentration metabolites threshold to exert health benefits, even in the so-called low-producers.This research was funded by Euromed S.A. (Mollet del Vallès, Barcelona, Spain).Peer reviewedMultidisciplinary Digital Publishing InstituteConsejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72]202520252021info:eu-repo/semantics/articlehttp://purl.org/coar/resource_type/c_6501Publisher's versioninfo:eu-repo/semantics/publishedVersionapplication/pdfhttp://hdl.handle.net/10261/411930reponame:DIGITAL.CSIC. Repositorio Institucional del CSICinstname:Consejo Superior de Investigaciones Científicas (CSIC)InglésÁvila-Gálvez, María Ángeles; Giménez-Bastida, J. A.; González-Sarrías, Antonio; Espín de Gea, Juan Carlos; 2021; Supplementary Materials: New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study [Dataset]; Multidisciplinary Digital Publishing Institute; https://doi.org/10.3390/antiox10030435https://doi.org/10.3390/antiox10030435Síinfo:eu-repo/semantics/openAccessoai:digital.csic.es:10261/4119302026-05-22T06:33:51Z |
| dc.title.none.fl_str_mv |
New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study |
| title |
New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study |
| spellingShingle |
New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study Ávila-Gálvez, María Ángeles Flavanones Gut microbiota Citrus Orange Hesperidin Lemon Eriocitrin Pharmacokinetics Hesperetin metabolites Eriodictyol metabolites |
| title_short |
New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study |
| title_full |
New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study |
| title_fullStr |
New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study |
| title_full_unstemmed |
New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study |
| title_sort |
New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study |
| dc.creator.none.fl_str_mv |
Ávila-Gálvez, María Ángeles Giménez-Bastida, J. A. González-Sarrías, Antonio Espín de Gea, Juan Carlos |
| author |
Ávila-Gálvez, María Ángeles |
| author_facet |
Ávila-Gálvez, María Ángeles Giménez-Bastida, J. A. González-Sarrías, Antonio Espín de Gea, Juan Carlos |
| author_role |
author |
| author2 |
Giménez-Bastida, J. A. González-Sarrías, Antonio Espín de Gea, Juan Carlos |
| author2_role |
author author author |
| dc.contributor.none.fl_str_mv |
Consejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72] |
| dc.subject.none.fl_str_mv |
Flavanones Gut microbiota Citrus Orange Hesperidin Lemon Eriocitrin Pharmacokinetics Hesperetin metabolites Eriodictyol metabolites |
| topic |
Flavanones Gut microbiota Citrus Orange Hesperidin Lemon Eriocitrin Pharmacokinetics Hesperetin metabolites Eriodictyol metabolites |
| description |
The intake of hesperidin-rich sources, mostly found in orange juice, can decrease cardiometabolic risk, potentially linked to the gut microbial phase-II hesperetin derivatives. However, the low hesperidin solubility hampers its bioavailability and microbial metabolism, yielding a high inter-individual variability (high vs. low-producers) that prevents consistent health-related evidence. Contrarily, the human metabolism of (lemon) eriocitrin is hardly known. We hypothesize that the higher solubility of (lemon) eriocitrin vs. (orange) hesperidin might yield more bioavailable metabolites than hesperidin. A randomized-crossover human pharmacokinetic study (n = 16) compared the bioavailability and metabolism of flavanones from lemon and orange extracts and postprandial changes in oxidative, inflammatory, and metabolic markers after a high-fat-high-sugars meal. A total of 17 phase-II flavanone-derived metabolites were identified. No significant biomarker changes were observed. Plasma and urinary concentrations of all metabolites, including hesperetin metabolites, were higher after lemon extract intake. Total plasma metabolites showed significantly mean lower Tmax (6.0 ± 0.4 vs. 8.0 ± 0.5 h) and higher Cmax and AUC values after lemon extract intake. We provide new insights on hesperetin-eriodictyol interconversion and naringenin formation from hesperidin in humans. Our results suggest that regular consumption of a soluble and eco-friendly eriocitrin-rich lemon extract could provide a circulating concentration metabolites threshold to exert health benefits, even in the so-called low-producers. |
| publishDate |
2021 |
| dc.date.none.fl_str_mv |
2021 2025 2025 |
| dc.type.none.fl_str_mv |
info:eu-repo/semantics/article http://purl.org/coar/resource_type/c_6501 Publisher's version info:eu-repo/semantics/publishedVersion |
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article |
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publishedVersion |
| dc.identifier.none.fl_str_mv |
http://hdl.handle.net/10261/411930 |
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http://hdl.handle.net/10261/411930 |
| dc.language.none.fl_str_mv |
Inglés |
| language_invalid_str_mv |
Inglés |
| dc.relation.none.fl_str_mv |
Ávila-Gálvez, María Ángeles; Giménez-Bastida, J. A.; González-Sarrías, Antonio; Espín de Gea, Juan Carlos; 2021; Supplementary Materials: New insights into the metabolism of the flavanones eriocitrin and hesperidin: A comparative human pharmacokinetic study [Dataset]; Multidisciplinary Digital Publishing Institute; https://doi.org/10.3390/antiox10030435 https://doi.org/10.3390/antiox10030435 Sí |
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info:eu-repo/semantics/openAccess |
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openAccess |
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application/pdf |
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Multidisciplinary Digital Publishing Institute |
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Multidisciplinary Digital Publishing Institute |
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reponame:DIGITAL.CSIC. Repositorio Institucional del CSIC instname:Consejo Superior de Investigaciones Científicas (CSIC) |
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Consejo Superior de Investigaciones Científicas (CSIC) |
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DIGITAL.CSIC. Repositorio Institucional del CSIC |
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DIGITAL.CSIC. Repositorio Institucional del CSIC |
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