Lupulone is a beta-acid that has been found in the hop plant, H. lupulus, and has diverse biological activities, including antibacterial, antioxidant, and anticarcinogenic properties.1,2,3 Lupulone is active against B. subtilis and S. aureus (MICs = 1 and 1.2 µg/ml, respectively), as well as T. b. brucei and L. m. mexicana (IC50s = 0.9 and 4.7 µg/ml, respectively).1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay and inhibits lipid peroxidation in rat brain homogenates (IC50s = 25 and 39 µM, respectively).4 It reduces proliferation, migration, and capillary tube formation in human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 2.5 to 50 µg/ml.5 Lupulone (40 µg/ml) activates the extrinsic apoptotic death pathway in SW480 and SW620 colon cancer cells.3
1.Teuber, M., and Schmalreck, A.F.Membrane leakage in Bacillus subtilis 168 induced by the hop constituents lupulone, humulone, isohumulone and humulinic acidArch. Mikrobiol.94(2)159-171(1973) 2.Bocquet, L., Sahpaz, S., Bonneau, N., et al.Phenolic compounds from Humulus lupulus as natural antimicrobial products: New weapons in the fight against methicillin resistant Staphylococcus aureus, Leishmania mexicana and Trypanosoma brucei strainsMolecules24(6)1024(2019) 3.Lamy, V., Roussi, S., Chaabi, M., et al.Lupulone, a hop bitter acid, activates different death pathways involving apoptotic TRAIL-receptors, in human colon tumor cells and in their derived metastatic cellsApoptosis13(10)1232-1242(2008) 4.Tagashira, M., Watanabe, M., and Uemitsu, N.Antioxidative activity of hop bitter acids and their analoguesBiosci. Biotechnol. Biochem.59(4)740-742(1995) 5.Siegel, L., Miternique-Grosse, A., Griffon, C., et al.Antiangiogenic properties of lupulone, a bitter acid of hop conesAnticancer Res.28(1A)289-294(2008)