Colupulone (Synonyms: NSC 650561)

Colupulone is a β-acid that has been found in H. lupulus and has diverse biological activities.^1,2,3 It activates the pregnane X receptor (PXR) in a reporter assay when used at concentrations of 1, 3, and 10 µM.¹ Dietary administration of colupulone (0.18% w/w) induces hepatic cytochrome P450 (CYP) isoform 3A (CYP3A) activity in mice.² It also decreases serum glucose levels in non-diabetic mice and increases serum glucose levels in db/db mice.³

1.Teotico, D.G., Bischof, J.J., Peng, L., et al.Structural basis of human pregnane X receptor activation by the hops constituent colupuloneMol. Pharmacol.74(6)1512-1520(2008) 2.Mannering, G.J., Shoeman, J.A., and Deloria, L.B.Identification of the antibiotic hops component, colupulone, as an inducer of hepatic cytochrome P-4503A in the mouseDrug Metab. Dispos.20(2)142-147(1992) 3.Mannering, G.J., Shoeman, J.A., and Shoeman, D.W.Effects of colupulone, a component of hops and brewers yeast, and chromium on glucose tolerance and hepatic cytochrome P450 in nondiabetic and spontaneously diabetic miceBiochem. Biophys. Res. Commun.200(3)1455-1462(1994)