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Tangeritin is a polymethoxylated flavone isolated from peels of citrus fruits. It inhibits signaling in cancer cells, reducing ERK phosphorylation and growth of estradiol-stimulated T47D breast cancer cells (IC50 ~ 3 μM)1 and blocking p38 MAPK, JNK, and Akt activation in interleukin-1β-stimulated human lung carcinoma A549 cells.2 Tangeritin activates the pregnane X receptor, inducing MDR1 expression in human colonic LS180 cancer cells at a concentration of 10 μM.3 It also inhibits growth of tumors and tumor implantation in lungs of mice inoculated with murine melanoma B16F10 cells.4 Tangeritin has been shown to protect against tunicamycin-induced cell death in isolated murine insulinoma MIN6 cells and in renal tubular epithelium in mice at a concentration of 10 μM.5 More recently, tangeritin has been found to significantly reduce serum total and LDL cholesterol and triacylglycerols in hypercholesteremic hamsters.6
1
Van Slambrouck, S., Parmar, V.S., Sharma, S.K., et al. Tangeretin inhibits extracellular-signal-regulated kinase (ERK) phosphorylation. FEBS Lett5791665-1669(2005).
2
Chen, K., Weng, M., and Lin, J. Tangeretin suppresses IL-1b-induced cyclooxygenase (COX)-2 expression through inhibition of p38 MAPK, JNK, and AKT activation in human lung carcinoma cells. Biochem Pharmacol73215-227(2007).
3
Satsu, H., Hiura, Y., Mochizuki, K., et al. Activation of pregnane X receptor and induction of MDR1 by dietary phytochemicals. J Agric Food Chem565366-5373(2008).
4
Conesa, C.M., Ortega, V.V., Gascón, M.J.Y., et al. Treatment of metastatic melanoma B16F10 by the flavonoids tangeretin, rutin, and diosmin. J Agric Food Chem536791-6797(2005).
5
Takano, K., Tabata, Y., Kitao, Y., et al. Methoxyflavones protect cells against endoplasmic reticulum stress and neurotoxin. Am J Physiol Cell Physiol292C353-C361(2007).
6
Kurowska, E.M., and Manthey, J.A. Hypolipidemic effects and absorption of citrus polymethoxylated flavones in hamsters with diet-induced hypercholesterolemia. J Agric Food Chem522879-2886(2004).
Kurowska, E.M., and Manthey, J.A. Hypolipidemic effects and absorption of citrus polymethoxylated flavones in hamsters with diet-induced hypercholesterolemia. J Agric Food Chem522879-2886(2004).
Takano, K., Tabata, Y., Kitao, Y., et al. Methoxyflavones protect cells against endoplasmic reticulum stress and neurotoxin. Am J Physiol Cell Physiol292C353-C361(2007).
Conesa, C.M., Ortega, V.V., Gascón, M.J.Y., et al. Treatment of metastatic melanoma B16F10 by the flavonoids tangeretin, rutin, and diosmin. J Agric Food Chem536791-6797(2005).
Satsu, H., Hiura, Y., Mochizuki, K., et al. Activation of pregnane X receptor and induction of MDR1 by dietary phytochemicals. J Agric Food Chem565366-5373(2008).
Chen, K., Weng, M., and Lin, J. Tangeretin suppresses IL-1b-induced cyclooxygenase (COX)-2 expression through inhibition of p38 MAPK, JNK, and AKT activation in human lung carcinoma cells. Biochem Pharmacol73215-227(2007).
Van Slambrouck, S., Parmar, V.S., Sharma, S.K., et al. Tangeretin inhibits extracellular-signal-regulated kinase (ERK) phosphorylation. FEBS Lett5791665-1669(2005).