Home Metabolism COX inhibitor - Apoptosis related activator - Acyltransferase inhibitor - CMV inhibitor Xanthohumol

Xanthohumol

Catalog No.S7889

For research use only.

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.

Xanthohumol Chemical Structure

CAS No. 6754-58-1

Selleck's Xanthohumol has been cited by 9 Publications

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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 Research:

[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 Research:

[3] [4]
  • Animal Models: CETP-Tg and C57BL/6N (wild-type) mice; TRAMP C57BL/6 mice
  • Dosages: 50 μg/mouse
  • Administration: p.o.

Solubility (25°C)

In vitro

 DMSO 70 mg/mL
(197.51 mM)
Water Insoluble
Ethanol '70 mg/mL

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.05% (w+w) xanthohumol powder in diet, or suspended in ethanol (2.5 mg+mL)
For best results, use promptly after mixing.

 13mg/mL

Chemical Information

Molecular Weight 354.4
Formula

C21H22O5
CAS No. 6754-58-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=CCC1=C(C(=C(C=C1O)OC)C(=O)C=CC2=CC=C(C=C2)O)O)C

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03735420 Active not recruiting Drug: Xanthohumol|Drug: Placebo oral capsule Healthy National University of Natural Medicine|Oregon State University|Pacific Northwest National Laboratory August 12 2019 Phase 1
NCT01367431 Completed Dietary Supplement: Xanthohumol Metabolic Syndrome Oregon State University|Oregon Health and Science University|National Center for Complementary and Integrative Health (NCCIH) August 2011 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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