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    InvivoChem Cat #: V1046
    CAS #: 6754-58-1Purity ≥98%

    Description: Xanthohumol, a naturally occuring prenylated chalcone compound isolated from hops (the female inflorescences of Humulus lupulus), is an inhibitor of COX-1 and COX-2 enzymatic activity and shows chemopreventive effects as well as anti-cancer and anti-angiogenic activities. It binds to the N domain of VCP, suppressing function and impairing autophagosome maturation. It inhibits growth of a wide variety of human cancer cell lines by inhibiting proliferation and inducing apoptosis. Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities.

    References: Mol Cancer Ther. 2002 Sep;1(11):959-69; Antiviral Res. 2004 Dec;64(3):189-94; PLoS One. 2012;7(11):e49415. 

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    Molecular Weight (MW)354.4
    CAS No.6754-58-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 70 mg/mL (197.5 mM)
    Water:<1 mg/mL
    Ethanol: 70 mg/mL (197.5 mM)
    Solubility (In vivo)0.05% (w+w) xanthohumol powder in diet, or suspended in ethanol (2.5 mg+mL): 13mg/mL
    SynonymsXanthohumol; (E)-1-[2,4-Dihydroxy-6-methoxy-3-(3-methylbut-2-enyl)phenyl]-3-(4-hydroxyphenyl)prop-2-en-1-one

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    In Vitro

    In vitro activity: Xanthohumol inhibits Cyp1A activity and induces QR activity in mouse hepatoma cell culture. Xanthohumol scavenges reactive oxygen species and inhibits superoxide anion radical and nitric oxide production. In addition, Xanthohumol prevents carcinogenesis via inhibition of DNA synthesis and induction of cell cycle arrest in S phase, apoptosis, and cell differentiation. Xanthohumol shows potent anti-HIV-1 activity.

    Kinase Assay: Inhibition of Cox-1 activity is measured by monitoring oxygen consumption during the conversion of arachidonic acid to PGs using a Clark-type O2-electrode. The reaction mixture contains ∼0.2 units Cox-1 in 100 μL of microsome fraction derived from ram seminal vesicles as a crude source of Cox-1 (specific activity 0.2–1 units/mg protein) or 0.23 units of recombinant human Cox-2 (specific activity 43 units/mg protein). For calculation, the rate of O2 consumption is compared with a DMSO control (100% activity). Piroxicam, a nonsteroidal anti-inflammatory drug, is used as positive inhibitory substance for Cox-1 activity with an IC50 of 0.35 ± 0.05 μM (n = 2). Alternatively, nimesulide, a Cox-2 specific inhibitor, inhibits Cox-2 activity by 52 ± 5.7% (n = 2) at a concentration of 50 μM.

    Cell Assay: HL-60 cells are maintained in RPMI 1640 supplemented with 10% FBS at 37°C in a 5% CO2 atmosphere. Log-phase cells with a population doubling time of 14–16 h are used for experiments. Serial 2-fold dilutions of compounds (dissolved in DMSO, final concentration 0.1%) in a final concentration range of 0.2–12.5 μM are prepared in 24-well plates using 1 ml of RPMI/well. Control wells obtain the same amount of solvent. Subsequently, 1 ml of the cell suspension is added to the wells. After 96 h, the experiment is evaluated. Cell numbers are counted using a Casy 1 TTC flow-cytometer. The proliferation of treated cells is expressed as a percentage in comparison with the solvent control.

    In VivoIn CETP-Tg mice, xanthohumol (p.o.) prevents cholesterol accumulation leading to atherosclerosis. In TRAMP mice, xanthohumol (p.o.) induces a decrease in the average weight of the urogenital (UG) tract, delays advanced tumor progression and inhibits the growth of poorly differentiated prostate carcinoma.
    Animal modelCETP-Tg and C57BL/6N (wild-type) mice; TRAMP C57BL/6 mice
    Formulation & DosageDissolved in 0.05% (w/w) xanthohumol powder in diet, or suspended in ethanol (2.5 mg/mL); 50 mg/kg/day; p.o. administration

    Mol Cancer Ther. 2002 Sep;1(11):959-69; Antiviral Res. 2004 Dec;64(3):189-94; PLoS One. 2012;7(11):e49415. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.


    Effect of xanthohumol on serum cholesterol and CETP activity. PLoS One. 2012;7(11):e49415.


    Expression analyses in mice liver and ab. aorta. PLoS One. 2012;7(11):e49415.


    Xanthohumol increased apoE protein expression in CETP-Tg mice after 18 weeks.

    Changes in cholesterol accumulation over 18 weeks. PLoS One. 2012;7(11):e49415.


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