包裝規(guī)格：
20mg in glass bottle
產(chǎn)品簡(jiǎn)介：
從啤酒花中分離到的黃酮類化合物，是?DGAT，COX-1?和?COX-2?的抑制劑，具有抗腫瘤，抗血管生成的作用。Xanthohumol 還具有抗牛病毒性腹瀉病毒 (BVDV)，鼻病毒，HSV-1，HSV-2?和 巨細(xì)胞病毒 (CMV) 的抗病毒活性。
溶解性：
DMSO :?83.33 mg/mL?(235.13 mM;?Need ultrasonic)
儲(chǔ)備液保存：
-80°C, 2 years
-20°C, 1 year
體內(nèi)實(shí)驗(yàn)：
1、請(qǐng)依序添加每種溶劑：10% DMSO→40%?PEG300→5%?Tween-80→45% saline
Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution
此方案可獲得 ≥ 2.08 mg/mL (5.87 mM，飽和度未知) 的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；向上述體系中加入50 μL Tween-80，混合均勻；然后繼續(xù)加入 450 μL生理鹽水定容至 1 mL。
2、請(qǐng)依序添加每種溶劑：10% DMSO→90% (20%?SBE-β-CD?in saline)
Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution
此方案可獲得 ≥ 2.08 mg/mL (5.87 mM，飽和度未知) 的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL?20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物濃度為內(nèi)部測(cè)試所得，實(shí)際溶液度可能與公布值有所偏差，屬于正常的批間細(xì)微差異現(xiàn)象。
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
靶點(diǎn)：
COX-1;COX-2;HSV-1;HSV-2;DGAT140 μM (IC50);DGAT240μM (IC50);CMV
體外研究：
Xanthohumol significantly attenuates ADP-induced blood platelet aggregation, and significantly reduces the expression of fibrinogen receptor (activated form of GPIIbIIIa) on platelets' surface.
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.
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.
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.
激酶實(shí)驗(yàn)：
Cox 活性的抑制：COX-1活性的抑制使用Clark型O2-電極通過(guò)監(jiān)測(cè)花生四烯酸轉(zhuǎn)化到PGs期間氧氣消耗量測(cè)量。反應(yīng)混合物包含來(lái)源于公羊精囊的100 μL線粒體碎片中的～0.2單元Cox-1作為Cox-1 (比活度0.2–1 units/mg蛋白質(zhì))的天然來(lái)源，或0.23單元重組人Cox-2 (比活度43 units/mg 蛋白質(zhì))。對(duì)于計(jì)算，O2消耗率與DMSO對(duì)照組(100% 活性)比較。Piroxicam，一種非甾體類抗炎化合物，用作Cox-1活性的陽(yáng)性抑制物質(zhì)，IC50為0.35 ± 0.05 μM (n = 2)?；蛘?，nimesulide，一種Cox-2特異性抑制劑，在50 μM濃度下抑制52 ± 5.7% (n = 2)的Cox-2活性。
細(xì)胞實(shí)驗(yàn)：
細(xì)胞系：HL-60細(xì)胞
濃度：12.5 μM
孵育時(shí)間：96 h
方法：HL-60細(xì)胞維持在RPMI 1640中，用10% FBS增補(bǔ)，置于37°C，5% CO2大氣環(huán)境下。對(duì)數(shù)期14–16 h細(xì)胞群體倍增時(shí)間用于進(jìn)行實(shí)驗(yàn)。連續(xù)2倍稀釋的化合物(在DMSO中溶解，終濃度為0.1%)以0.2–12.5 μM的終濃度范圍在24孔板中使用1 ml RPMI/孔制備。對(duì)照孔加入相同量的溶劑。隨后，將1 ml細(xì)胞懸浮液加入孔中。96小時(shí)后，評(píng)估實(shí)驗(yàn)。細(xì)胞數(shù)量使用Casy 1 TTC流式細(xì)胞計(jì)數(shù)儀計(jì)數(shù)。處理細(xì)胞的增殖表示為溶劑對(duì)照組的百分比。
動(dòng)物實(shí)驗(yàn)：
Animal Models：CETP-Tg 和 C57BL/6N (野生型)小鼠，TRAMP C57BL/6 小鼠
Dosages：50 μg/小鼠
Administration：p.o.
注意事項(xiàng)：
1、為了您的安全和健康，請(qǐng)穿實(shí)驗(yàn)服并戴一次性手套操作。
2、以上信息僅做參考交流之用。
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（ 母液濃度為 40 mg/mL ）, 如您需要配置的濃度超過(guò)該產(chǎn)品的溶解度，請(qǐng)先與我們客服聯(lián)系。
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