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Xanthohumol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Xanthohumol图片
CAS NO:6754-58-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
黄腐酚
产品介绍
Xanthohumol 是从啤酒花中分离到的黄酮类化合物,是DGATCOX-1和 COX-2 的抑制剂,具有抗肿瘤,抗血管生成的作用。Xanthohumol 还具有抗牛病毒性腹泻病毒 (BVDV),鼻病毒,HSV-1HSV-2和 巨细胞病毒 (CMV) 的抗病毒活性。
生物活性

Xanthohumol is one of the principalflavonoidsisolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT),COX-1andCOX-2, and shows anti-cancer and anti-angiogenic activities. Xanthohumol also has antiviral activity againstbovine viral diarrhea virus (BVDV),rhinovirus,HSV-1,HSV-2andcytomegalovirus (CMV).

IC50& Target[1][2][3][4][5]

COX-1

 

COX-2

 

HSV-1

 

HSV-2

 

DGAT1

40 μM (IC50)

DGAT2

40 μM (IC50)

CMV

 

体外研究
(In Vitro)

Xanthohumol significantly attenuates ADP-induced blood platelet aggregation, and significantly reduces the expression of fibrinogen receptor (activated form of GPIIbIIIa) on platelets' surface[1].
Xanthohumol (5-50 nM) reduces the frequency of spontaneously occurring Ca2+sparks and Ca2+waves in control myocytes and in cells subjected to Ca2+overload caused by: (1) exposure to low K+solutions, (2) periods of high frequency electrical stimulation, (3) exposures to isoproterenol or (4) caffeine. Xanthohumol (50-100 nM) reduces the rate of relaxation of electrically- or caffeine-triggered Ca2+transients, without suppressing ICa, but this effect is small and reversed by isoproterenol at physiological temperatures. Xanthohumol also suppresses the Ca2+content of the SR, and its rate of recirculation[2].
Treatment of endothelial cells with Xanthohumol leads to increased AMPK phosphorylation and activity. Functional studies using biochemical approaches confirm that AMPK mediates Xanthohumol anti-angiogenic activity. AMPK activation by Xanthohumol is mediated by CAMMKβ, but not LKB1. Analysis of the downstream mechanisms shows that Xanthohumol-induced AMPK activation reduces nitric oxide (NO) levels in endothelial cells by decreasing eNOS phosphorylation. Finally, AKT pathway is inactivated by Xanthohumol as part of its anti-angiogenic activity, but independently from AMPK, suggesting that these two signaling pathways proceed autonomously[3].
Xanthohumol significantly reduces cell viability and induces apoptosis via pro-caspase-3/8 cleavage and poly(ADP ribose) polymerase (PARP) degradation. Pro-caspase-9 cleavage, Bcl2 family expression changes, mitochondrial dysfunction, and intracellular ROS generation also participate in Xanthohumol-induced glioma cell death. Xanthohumol's inhibition of the IGFBP2/AKT/Bcl2 pathway via miR-204-3p targeting plays a critical role in mediating glioma cell death[4].

Clinical Trial
分子量

354.40

性状

Solid

Formula

C21H22O5

CAS 号

6754-58-1

结构分类
  • Flavonoids
  • Chalcones
  • Phenols
  • Polyphenols
来源
  • Plants
  • Moraceae
  • Humulus lupulusL.
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL(235.13 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8217 mL14.1084 mL28.2167 mL
5 mM0.5643 mL2.8217 mL5.6433 mL
10 mM0.2822 mL1.4108 mL2.8217 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.87 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.87 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。