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Quercetin is able to demethylate the p16INK4a gene promoter

Tan S, Wang C, Lu C, Zhao B, Cui Y, Shi X, Ma X

Chemotherapy, 2009

Abstract

BACKGROUND: Quercetin is a flavonoid found ubiquitously in nature. Studies in vitro and in vivo have suggested that quercetin may have a protective role against colon cancer.

METHODS: We selected the human colon cancer cell line RKO to investigate the effects of quercetin in vitro. RKO cells were treated with different concentrations of quercetin.

RESULTS: In comparison to the control, quercetin was able to inhibit the growth of RKO cells, as measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Untreated RKO cells demonstrated almost complete methylation of the p16INK4a gene. Hypermethylation of the p16INK4a gene was successfully reversed after 120 h of treatment with quercetin. Expression of the p16INK4a gene was restored in a concentration-dependent manner.

CONCLUSION: All these data suggest that quercetin has antitumor properties, probably via demethylation of the p16INK4a gene promoter.

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