Licochalcone (LA) is a novel estrogenic flavonoid isolated from PC-SPES composition herb licorice root that was reported to show significant antitumor activity in various malignant human cell lines. LA-elicited growth control and induction of apoptosis using androgen-independent p53-null PC-3 prostate cancer cells. LA induced modest level of apoptosis but had more pronounced effect on cell cycle progression arresting cells in G2/M, accompanied by suppression of cyclin B1 and cdc2. It also inhibited phosphorylation of Rb, specifically phosphorylation of S780 with no change of phosphorylation status of T821, decreased expression of transcription factor E2F concurrent with reduction of cyclin D1, down-regulation of CDKs 4 and 6, but increased cyclin E expression. These findings provide mechanistic explanation for LA activity and suggest that it may be considered as a chemopreventive agent and its anticancer properties should be further explored.
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