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dc.contributor.authorLarrosa, Mar-
dc.contributor.authorTomé-Carneiro, Joao-
dc.contributor.authorYáñez-Gascón, María J.-
dc.contributor.authorAlcántara, David-
dc.contributor.authorSelma, María Victoria-
dc.contributor.authorBeltrán Riquelme, David-
dc.contributor.authorGarcía-Conesa, María Teresa-
dc.contributor.authorUrbán, Cristina-
dc.contributor.authorLucas, Ricardo-
dc.contributor.authorTomás Barberán, Francisco-
dc.contributor.authorMorales, Juan C.-
dc.contributor.authorEspín de Gea, Juan Carlos-
dc.date.accessioned2011-07-04T07:19:35Z-
dc.date.available2011-07-04T07:19:35Z-
dc.date.issued2010-09-24-
dc.identifier.citationJournal of Medicinal of Chemistry 53(20): 7365-7376 (2010)es_ES
dc.identifier.issn0022-2623-
dc.identifier.other20866032-
dc.identifier.urihttp://hdl.handle.net/10261/37441-
dc.description12 páginas, 7 figuras, 2 esquemas.es_ES
dc.description.abstractThere is no pharmaceutical or definitive surgical cure for inflammatory bowel diseases (IBDs). The naturally occurring polyphenol resveratrol exerts anti-inflammatory properties. However, its rapid metabolism diminishes its effectiveness in the colon. The design of prodrugs to targeting active molecules to the colon provides an opportunity for therapy of IBDs. Herein we explore the efficacy of different resveratrol prodrugs and pro-prodrugs to ameliorate colon inflammation in the murine dextran sulfate sodium (DSS) model. Mice fed with a very low dose (equivalent to 10 mg for a 70 kg-person) of either resveratrol-3-O-(6′-O-butanoyl)-β-d-glucopyranoside (6) or resveratrol-3-O-(6′-O-octanoyl)-β-d-glucopyranoside (7) did not develop colitis symptoms and improved 6-fold the disease activity index (DAI) compared to resveratrol. Our results indicate that these pro-prodrugs exerted a dual effect: (1) they prevented the rapid metabolism of resveratrol and delivered higher quantities of resveratrol to the colon and (2) they reduced mucosal barrier imbalance and prevented diarrhea, which consequently facilitated the action of the delivered resveratrol in the colon mucosa.es_ES
dc.description.sponsorshipThis work was supported by the projects 200670F0131 (CSIC), CICYT-BFU2007-60576, and CSD2007-00063 (Fun-C-Food; Consolider Ingenio 2010). M.L. and R.L. are holders of a JAE-DOC grant from CSIC and M.V.S of a “Ramón y Cajal” grant from MCINN. J.T.C. is holder of a predoctoral grant from MCINN.es_ES
dc.language.isoenges_ES
dc.publisherAmerican Chemical Societyes_ES
dc.rightsclosedAccesses_ES
dc.subjectInflamatory bowel diseases (IBDs)es_ES
dc.subjectPolyphenoles_ES
dc.subjectAnti-inflammatoryes_ES
dc.subjectColones_ES
dc.subjectDextran suflate sodium (DSS)es_ES
dc.subjectResveratroles_ES
dc.titlePreventive Oral Treatment with Resveratrol Pro-prodrugs Drastically Reduce Colon Inflammation in Rodentses_ES
dc.typeartículoes_ES
dc.identifier.doi10.1021/jm1007006-
dc.description.peerreviewedPeer reviewedes_ES
dc.relation.publisherversionhttp://dx.doi.org/10.1021/jm1007006es_ES
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