Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12857/115519
Title: Resveratrol derivatives as a pharmacological tool
Authors: Biasutto, Lucia 
Mattarei, Andrea 
Azzolini, Michele
La Spina, Martina 
Sassi, Nicola 
Romio, Matteo 
Paradisi, Cristina 
Zoratti, Mario 
Keywords: bioefficacy;mitochondria-targeting;prodrugs;resveratrol
Keywords Plus: NF-KAPPA-B;IN-VIVO;TISSUE DISTRIBUTION;LIPOPHILIC CATIONS;VITIS-VINIFERA;MOUSE SKIN;PRODRUGS;MITOCHONDRIA;METABOLISM;CANCER
Mesh headings: Oxidative Stress;Prodrugs;Reactive Oxygen Species;Stilbenes
Secondary Mesh headings: Animals;Humans;Mitochondria;Resveratrol
Issue Date: 2017
Publisher: WILEY
Journal: Annals of the New York Academy of Sciences 
Abstract: 
Prodrugs of resveratrol are under development. Among the long-term goals, still largely elusive, are (1) modulating physical properties (e.g., water-soluble derivatives bearing polyethylene glycol chains), (2) changing distribution in the body (e.g., galactosyl derivatives restricted to the intestinal lumen), (3) increasing absorption from the gastrointestinal tract (e.g., derivatives imitating the natural substrates of endogenous transporters), and (4) hindering phase II metabolism (e.g., temporarily blocking the hydroxyls), all contributing to (5) increasing bioavailability. The chemical bonds that have been tested for functionalization include carboxyester, acetal, and carbamate groups. A second approach, which can be combined with the first, seeks to reinforce or modify the biochemical activities of resveratrol by concentrating the compound at specific subcellular sites. An example is provided by mitochondria-targeted derivatives. These proved to be pro-oxidant and cytotoxic in vitro, selectively killing fast-growing and tumor cells when supplied in the low micromolar range. This suggests the possibility of anticancer applications.
URI: http://hdl.handle.net/20.500.12857/115519
ISSN: 00778923
DOI: 10.1111/nyas.13401
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