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Quercetin Is Able to Demethylate the p16INK4a Gene Promoter

Tan S.a–d · Wang C.a–c · Lu C.a · Zhao B.a–c · Cui Y.a–c · Shi X.a–c · Ma X.a–c
aReproductive and Genetic Center of the National Research Institute for Family Planning, bGraduate School, Peking Union Medical College, and cWorld Health Organization Collaborating Centre for Research in Human Reproduction, Beijing, and dResearch Institute for Family Planning in Hunan Province, Changsha, China Chemotherapy 2009;55:6–10 (DOI:10.1159/000166383)


Background: Quercetin is a flavonoid found ubiquitously in nature. Studies in vitroand in vivohave 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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