2024-03-29T11:22:56Zhttp://digital.csic.es/dspace-oai/requestoai:digital.csic.es:10261/1636002018-04-14T00:56:35Zcom_10261_64com_10261_1col_10261_317
DIGITAL.CSIC
author
Falomir, Eva
author
Lucas, Ricardo
author
Peñalver, Pablo
author
Martí-Centelles, Rosa
author
Dupont, Alexia
author
Zafra-Gómez, Alberto
author
Carda, Miguel
author
Morales, Juan C.
2018-04-13T08:48:04Z
2018-04-13T08:48:04Z
2016-05-04
ChemBioChem
1439-4227
http://hdl.handle.net/10261/163600
10.1002/cbic.201600084
1439-7633
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.
eng
openAccess
Angiogenesis
Antiproliferation
Cytotoxicity
Metabolite
Prodrug
resveratrol
Cytotoxic, Antiangiogenic and Antitelomerase Activity of Glucosyl- and Acyl- Resveratrol Prodrugs and Resveratrol Sulfate Metabolites
preprint
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URL
https://digital.csic.es/bitstream/10261/163600/1/ChemBioChem2016_Falomir%20et%20al_just%20accept.pdf
File
MD5
5cc695e29c62a7c31b23c979d2a61319
471421
application/pdf
ChemBioChem2016_Falomir et al_just accept.pdf