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Cytotoxic, antiangiogenic and antitelomerase activity of glucosyl- and acyl- resveratrol prodrugs and resveratrol sulfate metabolites
dc.contributor.author | Falomir, Eva | |
dc.contributor.author | Lucas, Ricardo | |
dc.contributor.author | Peñalver, Pablo | |
dc.contributor.author | Martí-Centelles, Rosa | |
dc.contributor.author | Dupont, Alexia | |
dc.contributor.author | Zafra Gómez, Alberto | |
dc.contributor.author | Carda, Miguel | |
dc.contributor.author | Morales, Juan C. | |
dc.date.accessioned | 2016-09-19T09:12:28Z | |
dc.date.available | 2016-09-19T09:12:28Z | |
dc.date.issued | 2016-06 | |
dc.identifier.citation | FALOMIR, Eva, et al. Cytotoxic, antiangiogenic and antitelomerase activity of glucosyl‐and acyl‐resveratrol prodrugs and resveratrol sulfate metabolites. ChemBioChem, Volume 17, Issue 14, 2016. | ca_CA |
dc.identifier.uri | http://hdl.handle.net/10234/162655 | |
dc.description.abstract | Resveratrol (RES) is a natural polyphenol with relevant and varied biological activity. However, its low bioavailability and rapid metabolism to its glucuronate and sulfate conjugates has opened a debate on the mechanisms underlying its bioactivity. RES prodrugs are being developed to overcome these problems. We have synthesized a series of RES prodrugs and RES sulfate metabolites (RES-S) and evaluated their biological activities. RES glucosylated prodrugs (RES-Glc) were more cytotoxic in HT-29 and MCF-7 cells than RES itself whereas RES-S showed similar or higher cytotoxicity than RES. VEGF production was decreased by RES-Glc, and RES-disulfate (RES-diS) diminished it even more than RES. Finally, RES-Glc and RES-diS inhibited hTERT gene expression to a higher extent than RES. In conclusion, resveratrol prodrugs are promising candidates as anticancer drugs. In addition, RES-S showed distinct biological activity, thus indicating they are not simply RES reservoirs. | ca_CA |
dc.description.sponsorShip | Financial support has been granted by the Spanish Government (Ministerio de Economía y Competitividad, projects CTQ2011-27560 and CTQ2012-35360), by the Consellería d’Empresa, Universitat i Ciencia de la Generalitat Valenciana (projects PROMETEO/2013/027) and by the Universitat Jaume I (project PI-1B-2011-37). | ca_CA |
dc.format.extent | 5 p. | ca_CA |
dc.format.mimetype | application/pdf | ca_CA |
dc.language.iso | eng | ca_CA |
dc.relation.isPartOf | ChemBioChem, Volume 17, Issue 14, July 2016. | ca_CA |
dc.rights | Copyright © 1999-2016 John Wiley & Sons, Inc. All Rights Reserved | ca_CA |
dc.rights.uri | http://rightsstatements.org/vocab/InC/1.0/ | * |
dc.subject | resveratrol | ca_CA |
dc.subject | polyphenol | ca_CA |
dc.subject | prodrug | ca_CA |
dc.subject | metabolite | ca_CA |
dc.subject | sulfate | ca_CA |
dc.subject | cytotoxicity | ca_CA |
dc.subject | antiproliferation | ca_CA |
dc.subject | angiogenesis | ca_CA |
dc.title | Cytotoxic, antiangiogenic and antitelomerase activity of glucosyl- and acyl- resveratrol prodrugs and resveratrol sulfate metabolites | ca_CA |
dc.type | info:eu-repo/semantics/article | ca_CA |
dc.identifier.doi | http://dx.doi.org/10.1002/cbic.201600084 | |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | ca_CA |
dc.relation.publisherVersion | http://onlinelibrary.wiley.com/wol1/doi/10.1002/cbic.201600084/abstract | ca_CA |
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