Glucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.

<h4>Background</h4>Chronic oral quercetin reduces blood pressure and restores endothelial dysfunction in hypertensive animals. However, quercetin (aglycone) is usually not present in plasma, because it is rapidly metabolized into conjugated, mostly inactive, metabolites. The aim of the s...

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Autores principales:	Pilar Galindo, Isabel Rodriguez-Gómez, Susana González-Manzano, Montserrat Dueñas, Rosario Jiménez, Carmen Menéndez, Félix Vargas, Juan Tamargo, Celestino Santos-Buelga, Francisco Pérez-Vizcaíno, Juan Duarte
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2012
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/3e9aad156f1d4ea09eb2e72e99a16723
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spelling	oai:doaj.org-article:3e9aad156f1d4ea09eb2e72e99a167232021-11-18T07:25:32ZGlucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.1932-620310.1371/journal.pone.0032673https://doaj.org/article/3e9aad156f1d4ea09eb2e72e99a167232012-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/22427863/?tool=EBIhttps://doaj.org/toc/1932-6203<h4>Background</h4>Chronic oral quercetin reduces blood pressure and restores endothelial dysfunction in hypertensive animals. However, quercetin (aglycone) is usually not present in plasma, because it is rapidly metabolized into conjugated, mostly inactive, metabolites. The aim of the study is to analyze whether deconjugation of these metabolites is involved in the blood pressure lowering effect of quercetin.<h4>Methodology/principal findings</h4>We have analyzed the effects on blood pressure and vascular function in vitro of the conjugated metabolites of quercetin (quercetin-3-glucuronide, Q3GA; isorhamnetin-3-glucuronide, I3GA; and quercetin-3'-sulfate, Q3'S) in spontaneously hypertensive rats (SHR). Q3GA and I3GA (1 mg/kg i.v.), but not Q3'S, progressively reduced mean blood pressure (MBP), measured in conscious SHR. The hypotensive effect of Q3GA was abolished in SHR treated with the specific inhibitor of β-glucuronidase, saccharic acid 1,4-lactone (SAL, 10 mg/ml). In mesenteric arteries, unlike quercetin, Q3GA had no inhibitory effect in the contractile response to phenylephrine after 30 min of incubation. However, after 1 hour of incubation Q3GA strongly reduced this contractile response and this effect was prevented by SAL. Oral administration of quercetin (10 mg/Kg) induced a progressive decrease in MBP, which was also suppressed by SAL.<h4>Conclusions</h4>Conjugated metabolites are involved in the in vivo antihypertensive effect of quercetin, acting as molecules for the plasmatic transport of quercetin to the target tissues. Quercetin released from its glucuronidated metabolites could be responsible for its vasorelaxant and hypotensive effect.Pilar GalindoIsabel Rodriguez-GómezSusana González-ManzanoMontserrat DueñasRosario JiménezCarmen MenéndezFélix VargasJuan TamargoCelestino Santos-BuelgaFrancisco Pérez-VizcaínoJuan DuartePublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 7, Iss 3, p e32673 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Pilar Galindo Isabel Rodriguez-Gómez Susana González-Manzano Montserrat Dueñas Rosario Jiménez Carmen Menéndez Félix Vargas Juan Tamargo Celestino Santos-Buelga Francisco Pérez-Vizcaíno Juan Duarte Glucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.
description	<h4>Background</h4>Chronic oral quercetin reduces blood pressure and restores endothelial dysfunction in hypertensive animals. However, quercetin (aglycone) is usually not present in plasma, because it is rapidly metabolized into conjugated, mostly inactive, metabolites. The aim of the study is to analyze whether deconjugation of these metabolites is involved in the blood pressure lowering effect of quercetin.<h4>Methodology/principal findings</h4>We have analyzed the effects on blood pressure and vascular function in vitro of the conjugated metabolites of quercetin (quercetin-3-glucuronide, Q3GA; isorhamnetin-3-glucuronide, I3GA; and quercetin-3'-sulfate, Q3'S) in spontaneously hypertensive rats (SHR). Q3GA and I3GA (1 mg/kg i.v.), but not Q3'S, progressively reduced mean blood pressure (MBP), measured in conscious SHR. The hypotensive effect of Q3GA was abolished in SHR treated with the specific inhibitor of β-glucuronidase, saccharic acid 1,4-lactone (SAL, 10 mg/ml). In mesenteric arteries, unlike quercetin, Q3GA had no inhibitory effect in the contractile response to phenylephrine after 30 min of incubation. However, after 1 hour of incubation Q3GA strongly reduced this contractile response and this effect was prevented by SAL. Oral administration of quercetin (10 mg/Kg) induced a progressive decrease in MBP, which was also suppressed by SAL.<h4>Conclusions</h4>Conjugated metabolites are involved in the in vivo antihypertensive effect of quercetin, acting as molecules for the plasmatic transport of quercetin to the target tissues. Quercetin released from its glucuronidated metabolites could be responsible for its vasorelaxant and hypotensive effect.
format	article
author	Pilar Galindo Isabel Rodriguez-Gómez Susana González-Manzano Montserrat Dueñas Rosario Jiménez Carmen Menéndez Félix Vargas Juan Tamargo Celestino Santos-Buelga Francisco Pérez-Vizcaíno Juan Duarte
author_facet	Pilar Galindo Isabel Rodriguez-Gómez Susana González-Manzano Montserrat Dueñas Rosario Jiménez Carmen Menéndez Félix Vargas Juan Tamargo Celestino Santos-Buelga Francisco Pérez-Vizcaíno Juan Duarte
author_sort	Pilar Galindo
title	Glucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.
title_short	Glucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.
title_full	Glucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.
title_fullStr	Glucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.
title_full_unstemmed	Glucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.
title_sort	glucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.
publisher	Public Library of Science (PLoS)
publishDate	2012
url	https://doaj.org/article/3e9aad156f1d4ea09eb2e72e99a16723
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Glucuronidated quercetin lowers blood pressure in spontaneously hypertensive rats via deconjugation.

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