Synthesis and Radioprotective Properties of Pulvinic Acid Derivatives

A high‐throughput screening method has highlighted the marked antioxidant activity of some pulvinic acid derivatives (PADs) towards oxidation of thymidine, under γ and UV irradiation, and Fenton‐like conditions. Here, we report the synthesis of a series of new hydrophilic PADs and the evaluation of...

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Veröffentlicht in:ChemMedChem 2011-03, Vol.6 (3), p.561-569
Hauptverfasser: Le Roux, Antoine, Meunier, Stéphane, Le Gall, Thierry, Denis, Jean-Marc, Bischoff, Pierre, Wagner, Alain
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Sprache:eng
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Zusammenfassung:A high‐throughput screening method has highlighted the marked antioxidant activity of some pulvinic acid derivatives (PADs) towards oxidation of thymidine, under γ and UV irradiation, and Fenton‐like conditions. Here, we report the synthesis of a series of new hydrophilic PADs and the evaluation of their radioprotective efficacy in cell culture. Using a cell‐based fluorescent assay, we show that some of these compounds have a pronounced ability to prevent cell death caused by radiation and to allow the subsequent resumption of proliferation. Thus, PADs may be considered as a novel class of radioprotective agents. In pulvinic we trust? Norbadione A, a naturally occurring pulvinic acid, is known to exhibit radioprotective activity. We synthesized several hydrophilic derivatives and tested their radioprotective efficacy in cell cultures. Excellent protection and cell proliferation was observed several days following strong X‐ray irradiation, which suggests that pulvinic acid derivatives are a novel class of radioprotecting agents worth further evaluation.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201000391