Tangeretin

Tangeretin 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 Tangeretin 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 Tangeretin 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, tangeretin has been found to significantly reduce serum total and LDL cholesterol and triacylglycerols in hypercholesteremic hamsters.⁶

WARNING This product is not for human or veterinary use.

1. Van Slambrouck, S., Parmar, V.S., Sharma, S.K., et al. Tangeretin inhibits extracellular-signal-regulated kinase (ERK) phosphorylation. FEBS Lett. 579(7), 1665-1669 (2005).

2. Chen, K.H., Weng, M.S., and Lin, J.K. Tangeretin suppresses IL-1ß-induced cyclooxygenase (COX)-2 expression through inhibition of p38 MAPK, JNK, and AKT activation in human lung carcinoma cells. Biochem. Pharmacol. 73(2), 215-227 (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 Chem. 56(13), 5366-5373 (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 Chem. 53(17), 6791-6797 (2005).

5. Takano, K., Tabata, Y., Kitao, Y., et al. Methoxyflavones protect cells against endoplasmic reticulum stress and neurotoxin. Am. J. Physiol. Cell Physiol. 292(1), C353-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 Chem. 52(10), 2879-2886 (2004).