Total extract of Beta vulgaris var. cicla seeds versus its purified phenolic components: antioxidant activities and antiproliferative effects against colon cancer cells.

INTRODUCTION: Beta vulgaris var. cicla (BV) leaves contain chemopreventive compounds that have been investigated for new drug discovery. These compounds belong to the family of the apigenin-glycosides. Since the leaves are seasonal products containing high percentages of water, they are easily degradable during storage in fresh conditions. To be stored they require a drying process, consuming time and a large amount of energy. The extraction of apigenin-glycosides may also be conveniently performed from BV seeds, which represent a stable and year-long available biomass.

OBJECTIVES: The present report was undertaken to find a strategy of purification of bioactive flavonoids from BV seeds and test their ability to inhibit proliferation both on human colon cancer (RKO) cells and normal human fibroblasts (HF).

MATERIALS AND METHODS: The ethyl-acetate extract of BV seeds was fractionated on a Sephadex LH 20 column. A fraction of this extract, labeled as P4, exploited a marked antiproliferative activity on RKO cells. The components of P4 were purified on an RP₁₈ column chromatography and identified by HPLC-ESI-MS as 2,4,5-trihydroxybenzaldehyde, 2,5-dihydroxybenzaldehyde, vanillic acid, xylosylvitexin, glucopyranosyl-glucopyrasyl-rhamnetin and glucopyranosyl-xylosyl-rhamnetin. All of them were tested for cytostatic and cytotoxic activity on RKO and HF cells.

RESULTS: Xylosylvitexin exhibited the strongest antiproliferative activity on RKO cells, together with an enhancement of the apoptosis, an increase of cells in the G₁ phase and a reduction of cells in the S phase; on the contrary, the proliferation of HF was significantly stimulated.

CONCLUSION: Xylosylvitexin is the main and more efficient chemopreventive compound in BV seeds, but the natural cocktail of molecules, represented by P4 fraction, showed a better compromise between the antiproliferative activity on RKO cells and the enhancement of HF proliferation.