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Título: | Cytotoxic, Antiangiogenic and Antitelomerase Activity of Glucosyl- and Acyl- Resveratrol Prodrugs and Resveratrol Sulfate Metabolites |
Autor: | Falomir, Eva; Lucas, Ricardo CSIC; Peñalver, Pablo CSIC ORCID; Martí-Centelles, Rosa; Dupont, Alexia; Zafra-Gómez, Alberto; Carda, Miguel; Morales, Juan C. | Palabras clave: | Angiogenesis Antiproliferation Cytotoxicity Metabolite Prodrug resveratrol |
Fecha de publicación: | 4-may-2016 | Editor: | John Wiley & Sons | Citación: | ChemBioChem | Resumen: | 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. | Versión del editor: | https://onlinelibrary.wiley.com/doi/full/10.1002/cbic.201600084#support-information-section | URI: | http://hdl.handle.net/10261/163600 | DOI: | 10.1002/cbic.201600084 | ISSN: | 1439-4227 | E-ISSN: | 1439-7633 |
Aparece en las colecciones: | (IPBLN) Artículos |
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ChemBioChem2016_Falomir et al_just accept.pdf | 460,37 kB | Adobe PDF | Visualizar/Abrir |
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