Xanthohumol, also known as 2', 4, 4'-trihydroxy-6'-methoxy-3'-prenylchalcone or desmethylxanthohumol, is a member of the class of compounds known as 3-prenylated chalcones. It inhibits COX-1 and COX-2 activity and shows chemopreventive effects.

DGAT-1:40 μM (IC50), DGAT-2:40 μM (IC50)

Xanthohumol抑制小鼠肝癌细胞培养中的Cyp1A活性并诱导QR活性。Xanthohumol清除活性氧物种，抑制超氧阴离子自由基和一氧化氮的产生。此外，Xanthohumol通过抑制DNA合成、诱导细胞周期在S期停滞、凋亡及细胞分化来阻止癌症的发生。[1] Xanthohumol还显示出强大的抗HIV-1活性。[2]

在CETP-Tg小鼠中，黄腐酚（p.o.）阻止胆固醇积聚导致动脉粥样硬化。[3] 在TRAMP小鼠中，黄腐酚（p.o.）促成尿生殖道（UG）平均重量下降, 延缓高级肿瘤进展并抑制低分化前列腺癌的生长。[4]

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.

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.(Only for Reference)