产品说明书
Xanthohumol
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同义名 : | - |
| CAS号 : | 6754-58-1 | |
| 货号 : | A139015 | |
| 分子式 : | C21H22O5 | |
| 纯度 : | 99% | |
| 分子量 : | 354.396 | |
| MDL号 : | MFCD00210576 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 85 mg/mL(239.84 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | 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. Xanthohumol significantly attenuates ADP-induced blood platelet aggregation, and significantly reduces the expression of fibrinogen receptor (activated form of GPIIbIIIa) on platelets' surface[3]. 5-50 nM xanthohumol reduced the frequency of spontaneously occurring Ca2+ sparks (>threefold) and Ca2+ waves in control myocytes and in cells subjected to Ca2+ overload caused by the following: 1) exposure to low K+ solutions, 2) periods of high frequency electrical stimulation, 3) exposures to isoproterenol, or 4) caffeine. At room temperatures, 50-100 nM xanthohumol reduced the rate of relaxation of electrically- or caffeine-triggered Ca2+transients, without suppressing ICa, but this effect was small and reversed by isoproterenol at physiologic temperatures. Xanthohumol also suppressed the Ca2+ content of the SR and its rate of recirculation[4]. The anti-angiogenic activity of XN was more potent than epigallocatechin-3-gallate (EGCG). Treatment of endothelial cells with XN led to increased AMPK (5' adenosine monophosphate-activated protein kinase) phosphorylation and activity[5]. XN significantly reduced cell viability and induced apoptosis via pro-caspase-3/8 cleavage and poly(ADP ribose) polymerase (PARP) degradation[6]. In addition, a xanthohumol-enriched hop extract displayed a weak to moderate antiviral activity against BVDV (bovine viral diarrhea virus) (therapeutic index (TI)=6.0), HSV-2 (TI=>5.3), Rhino (TI=4.0) and HSV-1 (TI=>1.9) with IC(50) values in the low microg/ml range. Xanthohumol accounted for the antiviral activity observed in the xanthohumol-enriched hop extract against BVDV, HSV-1 (herpes simplex virus type 1) and HSV-2. Xanthohumol also showed antiviral activity against CMV (cytomegalovirus), suggesting that it might have a generalized anti-herpesvirus antiviral activity. Again, superior antiviral activity was observed with the xanthohumol isomer against CMV[7]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02848430 | Food-Drug Interactions | Not Applicable | Active, not recruiting | October 18, 2018 | United States, Illinois ... 展开 >> University of Illinois at Chicago Chicago, Illinois, United States, 60612 收起 << |
| NCT01982734 | Pharmacokinetics of New Curcum... 展开 >>in Formulations Safety of New Curcumin Formulations 收起 << | Early Phase 1 | Completed | - | Germany ... 展开 >> University of Hohenheim Stuttgart, Baden-Württemberg, Germany, 70599 收起 << |
| NCT03561116 | Metabolic Syndrome | Not Applicable | Recruiting | October 2018 | Portugal ... 展开 >> Medical Faculty of University of Porto Recruiting Porto, Portugal, 4200-319 Contact: Raquel Soares, PhD (+351)225513624 raqsoa@med.up.pt 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.82mL 0.56mL 0.28mL |
14.11mL 2.82mL 1.41mL |
28.22mL 5.64mL 2.82mL |
| 参考文献 |
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