Xanthohumol

Catalog No.S7889 Batch:S788901

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Technical Data

Formula

C21H22O5
Molecular Weight 354.4 CAS No. 6754-58-1
Solubility (25°C)* In vitro DMSO 70 mg/mL (197.51 mM)
Ethanol 70 mg/mL (197.51 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1.
Targets
COX-1 [1] COX-2 [1] DGAT1 [5]
(Cell-free assay)		 DGAT2 [5]
(Cell-free assay)
40 μM 40 μM
In vitro

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. [1] Xanthohumol shows potent anti-HIV-1 activity. [2]
In vivo

In CETP-Tg mice, xanthohumol (p.o.) prevents cholesterol accumulation leading to atherosclerosis. [3] 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. [4]

Protocol (from reference)

Kinase Assay:

[1]
  • Inhibition of Cox Activity

    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:

[1]
  • Cell lines

    HL-60 cells

  • Concentrations

    12.5 μM

  • Incubation Time

    96 h

  • Method

    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.
Animal Study:

[3] [4]
  • Animal Models

    CETP-Tg and C57BL/6N (wild-type) mice; TRAMP C57BL/6 mice

  • Dosages

    50 μg/mouse

  • Administration

    p.o.

Selleck's Xanthohumol has been cited by 10 publications

Eeyarestatin I, an inhibitor of the valosin-containing protein, exhibits potent virucidal activity against the flaviviruses [ Antiviral Res, 2022, 207:105416] PubMed: 36113629
Xanthohumol Protects the Rat Myocardium against Ischemia/Reperfusion Injury-Induced Ferroptosis [ Oxid Med Cell Longev, 2022, 2022:9523491] PubMed: 35082973
Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease [ Int J Mol Sci, 2021, 22(22)12134] PubMed: 34830015
Xanthohumol targets the ERK1/2‑Fra1 signaling axis to reduce cyclin D1 expression and inhibit non‑small cell lung cancer [ Oncol Rep, 2020, 44(4):1365-1374] PubMed: 32945473
Xanthohumol-suppresses-glioblastoma-via-modulation-of-Hexokinase-2-mediated-glycolysis. [ J-Cancer, 2020, 6;11-14-:4047-4058] PubMed: 32368287
An antiviral drug screening system for enterovirus 71 based on an improved plaque assay: A potential high-throughput method [ J Med Virol, 2019, 91(8):1440-1447] PubMed: 30900754
Xanthohumol inhibits colorectal cancer cells via downregulation of Hexokinases II-mediated glycolysis. [ Int J Biol Sci, 2019, 15(11):2497-2508] PubMed: 31595166
Xanthohumol increases death receptor 5 expression and enhances apoptosis with the TNF-related apoptosis-inducing ligand in neuroblastoma cell lines [ PLoS One, 2019, 14(3):e0213776] PubMed: 30870485
Cholesterol Homeostatic Regulator SCAP-SREBP2 Integrates NLRP3 Inflammasome Activation and Cholesterol Biosynthetic Signaling in Macrophages. [ Immunity, 2018, 49(5):842-856] PubMed: 30366764
Antiproliferative and apoptotic effects of xanthohumol in cholangiocarcinoma. [ Oncotarget, 2017, 8(50):88069-88078] PubMed: 29152142

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SHIPPING AND STORAGE
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