Xanthohumol, the chalcone from beer hops (Humulus lupulus L.), is the ligand for farnesoid X receptor and ameliorates lipid and glucose metabolism in KK-A mice

Modification of the cysteine residues in IκBα kinase and NF-κB (p65) by xanthohumol leads to suppression of NF-κB–regulated gene products and potentiation of apoptosis in leukemia cells

“…36 In addition, researchers have shown that XN is a natural ligand for FXR and can activate FXR and modulate genes involved in lipid and glucose metabolism. 22 We sought to determine whether the effects of XN on the NF-B pathway are mediated through interaction with FXR. First, we used Western blot analysis to examine the expression of FXR in different cell lines used in our studies and in those known to express FXR (such as MCF-7).…”

“…Furthermore, this agent inhibits phase 1 cytochrome P450 enzyme, which is involved in metabolic activation of carcinogens 20 and induces phase 2 enzyme NAD(P)H:quinone reductase. 21 XN was found to activate the farnesoid X receptor (FXR), 22 inhibits triglyceride and apolipoprotein B secretion, 23 and exhibits antidiabetic activity through the inhibition of lipid and glucose metabolism. 22 Because the ability of XN to control cellular proliferation, cell survival, invasion, angiogenesis, and inflammation is closely associated with expression of gene products regulated by NF-B, we postulated that XN must mediate most of these effects by regulating the NF-B signaling cascade.…”

“…21 XN was found to activate the farnesoid X receptor (FXR), 22 inhibits triglyceride and apolipoprotein B secretion, 23 and exhibits antidiabetic activity through the inhibition of lipid and glucose metabolism. 22 Because the ability of XN to control cellular proliferation, cell survival, invasion, angiogenesis, and inflammation is closely associated with expression of gene products regulated by NF-B, we postulated that XN must mediate most of these effects by regulating the NF-B signaling cascade. Thus, in this study, we investigated in detail the effects of XN on different steps leading to NF-B activation, NF-B regulation of gene products, and NF-Bregulated cellular responses.…”

Effects of Xanthohumol-rich Extract from the Hop on Fatty Acid Metabolism in Rats Fed a High-fat Diet

“…Xanthohumol also acts on farnesoid X receptor through a selective bile acid receptor modulator, such as guggulsterone or polyunsaturated fatty acids, and thereby ameliorates lipid and glucose metabolism in KK-A y mice 10 .…”

Drink your prevention: beverages with cancer preventive phytochemicals

“…Moreover, XN shows a potential role in the prevention of bonedestructive diseases. 62 In addition, XN activates the farnesoid X receptor 63 and impairs glucose and lipid metabolism. The anti-inflammatory and antioxidant properties of XN have been extensively documented.…”