Nobiletin 是一种来自柑橘皮的聚甲氧基黄酮,可改善记忆力丧失,是一种RORs激动剂。Nobiletin 可以降低分化的 C2C12 肌管中的ROS的水平,并具有抗炎和抗癌特性,包括抗血管生成,抗增殖,抗转移和诱导细胞凋亡。
生物活性 | Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is aretinoid acid receptor-related orphan receptors (RORs)agonist. Nobiletin can reducereactive oxygen species(ROS)levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and inducedapoptosis[1][2][3][4]. |
IC50& Target | Retinoid acid receptor-related orphan receptors (RORs)[1]; reactive oxygen species (ROS)[1]; apoptosis[2] |
体外研究 (In Vitro) | Nobiletin (0-100 μM; 24 hours; U2OS and HOS cells) treatment progressively reduces protein expressions of MMP-2 and MMP-9. In U2OS and HOS cells, Nobiletin considerably reduces the phosphorylation of p-IKKα/β and p-IκBα, and protein expression of NF-κB in the cell nuclear fraction with the concomitant increase of the NF-κB expression in the cytosolic fraction. Nobiletin down-regulates the p-CREB and the SP-1 expressions in the nuclear fraction, whereas Nobiletin does not affect c-Jun and c-Fos expressions[1]. Nobiletin (0-100 μM; 24 hours; U2OS and HOS cells) treatment significantly reduces mRNA expressions of MMP-2 and MMP-9 dose-dependently in U2OS and HOS cells[1].
Western Blot Analysis[1] Cell Line: | U2OS and HOS cells | Concentration: | 0 μM, 25 μM, 50 μM, 75 μM, 100 μM | Incubation Time: | 24 hours | Result: | Progressively reduced protein expressions of MMP-2 and MMP-9. Considerably reduced the phosphorylation of p-IKKα/β and p-IκBα, and protein expression of NF-κB in the cell nuclear fraction with the concomitant increase of the NF-κB expression in the cytosolic fraction. Down-regulated the p-CREB and the SP-1 expressions in the nuclear fraction in U2OS and HOS cells. |
RT-PCR[1] Cell Line: | U2OS and HOS cells | Concentration: | 0 μM, 25 μM, 50 μM, 75 μM, 100 μM | Incubation Time: | 24 hours | Result: | Significantly reduced mRNA expressions of MMP-2 and MMP-9 dose-dependently in U2OS and HOS cells. |
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体内研究 (In Vivo) | Nobiletin (0.1% of regular diet; oral administration; daily; for 20 weeks; male C57BL/6 mice) treatment restores glucose homeostasis and promots energy expenditure and circadian activity in aged mice[2].
Animal Model: | 20- to 22-month-old male C57BL/6 mice[2] | Dosage: | 0.1% of regular diet | Administration: | Oral administration; daily; for 20 weeks | Result: | Fully restored glucose tolerance in aged mice, and increased basal body temperature and cold tolerance in aged mice. Led to a twofold increase in distance run/day on voluntary wheels compared with aged regular diet-fed mice during the active phase. |
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来源 | - Plants
- Rutaceae
- Citrus reticulataBlanco
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(124.26 mM;Need ultrasonic) 配制储备液 1 mM | 2.4852 mL | 12.4258 mL | 24.8515 mL | 5 mM | 0.4970 mL | 2.4852 mL | 4.9703 mL | 10 mM | 0.2485 mL | 1.2426 mL | 2.4852 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 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.21 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 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。 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.17 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.17 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.17 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.17 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 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 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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