Artículo
Cytotoxic, Antiangiogenic and Antitelomerase Activity of Glucosyl- and Acyl- Resveratrol Prodrugs and Resveratrol Sulfate Metabolites
Autor/es | Falomir, Eva
Lucas Rodríguez, Ricardo Peñalver, Pablo Martí Centelles, Rosa Dupont, Alexia Zafra-Gómez, Alberto Carda, Miguel Morales, Juan C. |
Departamento | Universidad de Sevilla. Departamento de Química Orgánica y Farmacéutica |
Fecha de publicación | 2016 |
Fecha de depósito | 2022-07-11 |
Publicado en |
|
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 ... 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. |
Agencias financiadoras | Ministerio de Economía y Competitividad (MINECO). España Generalitat Valenciana Universitat Jaume I |
Identificador del proyecto | CTQ2011–27560
CTQ2012–35360 PROME-TEO/2013/027 PI-1B-2011–37 |
Cita | Falomir, 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. |
Ficheros | Tamaño | Formato | Ver | Descripción |
---|---|---|---|---|
Cytotoxic antiangiogenic and ... | 713.4Kb | [PDF] | Ver/ | |