The flavones and flavonoids are a widespread group of natural products with a variety of reported beneficial health effects. Flavonoids have been implicated as possible active agents in the dietary benefits of citrus fruits. Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. The EC50 for these responses is approximately 50 µM.1 Hesperetin also inhibits histamine release from IgE-challenged RBL-2H3 cells, with a potency comparable to the commercial anti-allergy drug azelastine.2
1
Wilcox, L.J., Borradaile, N.M., de Dreu, L.E., et al. Secretion of hepatocyte apoB is inhibited by the flavonoids, naringenin and hesperetin, via reduced activity and expression of ACAT2 and MTP. J Lipid Res42725-734(2001).
2
Lee, N., Choi, S., Park, S., et al. Antiallergic activity of hesperidin is activated by intestinal microflora. Pharmacology71174-180(2004).
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COc1ccc(cc1O)C1CC(=O)c2c(cc(O)cc2O)O1
Background Reading
Wilcox, L.J., Borradaile, N.M., de Dreu, L.E., et al. Secretion of hepatocyte apoB is inhibited by the flavonoids, naringenin and hesperetin, via reduced activity and expression of ACAT2 and MTP. J Lipid Res42725-734(2001).
Lee, N., Choi, S., Park, S., et al. Antiallergic activity of hesperidin is activated by intestinal microflora. Pharmacology71174-180(2004).
Hesperetin is available in the following screening
library: