Cytotoxic, antiangiogenic and antitelomerase activity of glucosyl- and acyl- resveratrol prodrugs and resveratrol sulfate metabolites
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Other documents of the author: Falomir, Eva; Lucas, Ricardo; Peñalver, Pablo; Martí-Centelles, Rosa; Dupont, Alexia; Zafra Gómez, Alberto; Carda, Miguel; Morales, Juan C.
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comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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Cytotoxic, antiangiogenic and antitelomerase activity of glucosyl- and acyl- resveratrol prodrugs and resveratrol sulfate metabolitesAuthor (s)
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2016-06Bibliographic 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.Type
info:eu-repo/semantics/articlePublisher version
http://onlinelibrary.wiley.com/wol1/doi/10.1002/cbic.201600084/abstractSubject
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 ... [+]
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. [-]
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ChemBioChem, Volume 17, Issue 14, July 2016.Rights
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