2022-07-112022-07-112016Falomir, E., Lucas Rodríguez, R., Peñalver, P., Martí Centelles, R., Dupont, A., Zafra-Gómez, A.,...,Morales, J.C. (2016). Cytotoxic, Antiangiogenic and Antitelomerase Activity of Glucosyl- and Acyl- Resveratrol Prodrugs and Resveratrol Sulfate Metabolites. ChemBioChem, 17, 1343-1348.1439-42271439-7633https://hdl.handle.net/11441/135227Resveratrol (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.application/pdf6 p.engAttribution-NonCommercial-NoDerivatives 4.0 Internacionalhttp://creativecommons.org/licenses/by-nc-nd/4.0/AngiogenesisAntiproliferationCytotoxicityMetaboliteProdrugResveratrolinfo:eu-repo/semantics/articleinfo:eu-repo/semantics/openAccess10.1002/cbic.201600084