Home Metabolism COX inhibitor - Apoptosis related activator - Acyltransferase inhibitor - CMV inhibitor Xanthohumol For research use only.

Xanthohumol

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

Xanthohumol Chemical Structure

CAS No. 6754-58-1

Purity & Quality Control

Xanthohumol Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

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
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]
Kinase Assay 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). CP-16171, 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 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.
In Vivo
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]
Animal Research Animal Models CETP-Tg and C57BL/6N (wild-type) mice; TRAMP C57BL/6 mice
Dosages 50 μg/mouse
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06225258 Recruiting
Septic Shock|Pneumonia|ARDS
Medical University of Lublin
 May 9 2023 Phase 2
NCT03735420 Active not recruiting
Healthy
National University of Natural Medicine|Oregon State University|Pacific Northwest National Laboratory
 August 12 2019 Phase 1
NCT01367431 Completed
Metabolic Syndrome
Oregon State University|Oregon Health and Science University|National Center for Complementary and Integrative Health (NCCIH)
 August 2011 --

Chemical Information & Solubility

Molecular Weight 354.4 Formula

C21H22O5
CAS No. 6754-58-1 SDF Download Xanthohumol SDF
Smiles CC(=CCC1=C(C(=C(C=C1O)OC)C(=O)C=CC2=CC=C(C=C2)O)O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 70 mg/mL ( (197.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 70 mg/mL

Water : Insoluble


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