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7423628 
Journal Article 
Review 
Resveratrol derivatives as a pharmacological tool 
Biasutto, L; Mattarei, A; Azzolini, M; La Spina, M; Sassi, N; Romio, M; Paradisi, C; Zoratti, M; , 
2017 
Yes 
Annals of the New York Academy of Sciences
ISSN: 0077-8923
EISSN: 1749-6632 
WILEY 
HOBOKEN 
1403 
1 
27-37 
English 
28675763 
WOS:000411766400003 
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. 
Bioefficacy; Mitochondria-targeting; Prodrugs; Resveratrol; acetal derivative; carbamic acid derivative; carbonic acid derivative; carboxyester; carboxyl group; ester derivative; inorganic acid; prodrug; resveratrol; sulfonic acid derivative; unclassified drug; prodrug; reactive oxygen metabolite; resveratrol; stilbene derivative; biological activity; drug absorption; drug activity; drug efficacy; drug mechanism; human; mitochondrion; nonhuman; pharmacological parameters; Review; animal; drug effects; metabolism; oxidative stress; Animals; Humans; Mitochondria; Oxidative Stress; Prodrugs; Reactive Oxygen Species; Stilbenes 
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