Flavonoids Are Potential Inhibitors of Glucose Uptake in U937 Cells

Flavonoids are a group of polyphenolic compounds ubiquitously found in plants including fruits, and vegetables. Broad ranges of the biological activities of flavonoids have been reported using in vitro studies. I report that several natural flavonoids blocked glucose uptake in myelocytic U937 cells. Although there were some variations in the blocking activity of individual flavonoids, approximately half of the glucose uptake was blocked by flavonoids at the concentrations of 8-50 microM. The decreasing order of the blocking activity was fisetin >/= myricetin >/= quercetin >/= apigenin > genistein > cyanidin > daidzein >/= hesperetin > naringenin > catechin. Fisetin showed approximately 50% inhibition of glucose uptake at a concentration of 8 microM. Similar patterns of the inhibition were observed in lymphocytic Jurkat cells. Fisetin and quercetin inhibited glucose transport in a competitive manner. K(i) values for fisetin and quercetin were proximately 9 and 12 microM, respectively. This study showed that some types of natural flavonoids block glucose uptake in U937 cells and that natural flavonoids could be used as alternative blockers of glucose uptake in vitro.