<abstract xmlns="http://www.w3.org/1999/xhtml"> Quercetin is a natural polyphenol with proven health beneficial activities. In this study 15 new quercetin derivatives were prepared with the aim to enhance their bioavailability. Modification of their physicochemical properties could herewith improve the action in cells. The prepared compounds were tested for their antioxidant and cytotoxic activity. The ability to scavenge free radicals as well as ferric reducing antioxidant power of the new derivatives was not better than that of unmodified quercetin. But for acetylated esters a better cytotoxic activity was found on human cervical cancer cells HeLa than for the initial molecule. The best effect revealed chloronaphtoquinone quercetin (IC50=13.2 μM). For this compound comparable cytotoxic action on non-cancer murine fibroblast cells was detected (IC50=16.5 μM). The obtained results indicate that appropriate lipophilization of the quercetin molecule could improve its cytotoxic action in cells, probably due to its enhanced bioavailability</abstract>

Quercetin is a natural polyphenol with proven health beneficial activities. In this study 15 new quercetin derivatives were prepared with the aim to enhance their bioavailability. Modification of their physicochemical properties could herewith improve the action in cells. The prepared compounds were tested for their antioxidant and cytotoxic activity. The ability to scavenge free radicals as well as ferric reducing antioxidant power of the new derivatives was not better than that of unmodified quercetin. But for acetylated esters a better cytotoxic activity was found on human cervical cancer cells HeLa than for the initial molecule. The best effect revealed chloronaphtoquinone quercetin (IC50=13.2 μM). For this compound comparable cytotoxic action on non-cancer murine fibroblast cells was detected (IC50=16.5 μM). The obtained results indicate that appropriate lipophilization of the quercetin molecule could improve its cytotoxic action in cells, probably due to its enhanced bioavailability

Antioxidant action and cytotoxicity on HeLa and NIH-3T3 cells of new quercetin derivatives

Institute of Biochemistry, Nutrition and Health Protection, Faculty of Chemical and Food Technology, Slovak University of Technology, Bratislava, Slovakia

Eurofins Bel/Novamann s.r.o., Nové Zámky, Slovakia

Interdisciplinary Toxicology

Quercetin is a natural polyphenol with proven health beneficial activities. In this study 15 new quercetin derivatives were prepared with the aim to enhance...

Antioxidant action and cytotoxicity on HeLa and NIH-3T3 cells of new quercetin derivatives

Publié en ligne: 11 mars 2014

Pages: 209 - 216

DOI: https://doi.org/10.2478/intox-2013-0031

This content is open access.