| CAS |
No.500-38-9 |
| 中文名称 |
去甲二氢愈创木酸(10mM in DMSO,无菌） |
| 英文名称 |
Nordihydroguaiaretic Acid(10mM in DMSO，Sterile） |
| 分子式 |
C18H22O4 |
| 分子量 |
302.37 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
5-Lipoxygenase |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
Nordihydroguaiaretic Acid是一种 5-脂氧合酶 (5LOX)和酪氨酸激酶抑制剂。 |
| 生物活性 |
Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC50=8 μM) and tyrosine kinase inhibitor.[1-3] |
| In Vitro |
天然的双酚 Nordihydroguaiaretic acid (NDGA) 是一种来自杂酚油植物 (Larrea tridentata：Zygophyllaceae) 的选择性 5LOX 抑制剂。抑制 5LOX 的天然双酚 Nordihydroguaiaretic acid 是一种非常有效、无毒的 TNFα 刺激的小胶质细胞激活拮抗剂。Nordihydroguaiaretic acid 在体外的效力大约是 Minocycline 的 6 倍，IC50 值为 8±3 μM，在 100 μM 时无毒性。在 800 nM Nordihydroguaiaretic acid 下观察到显著的 NO2- 抑制。对于天然和合成的 Nordihydroguaiaretic acid 以及 Nordihydroguaiaretic acid 的乙酰酯，观察到类似的功效。Nordihydroguaiaretic acid 还抑制 EOC-20 细胞受 TNFα 刺激的 PGE 生成2，IC50 为 841 nM[1]。前列腺素 E1 和 Nordihydroguaiaretic acid (NDGA) 对癌细胞系的增殖作用，HepG2 细胞系分别用不同剂量的两种化合物和阳性化合物 8-苯胺基-1-萘磺酸盐 (ANS) 处理 24 小时和通过 MTT 测定检查细胞活力。ANS 表现出剂量依赖性抑制作用 (0、10、30、50、80、100、120 和 150 μM)，估计的 IC50 为 25.888 μM。在 0、30、60、80、100、120、140 μM 不同浓度下，前列腺素 E1 和 Nordihydroguaiaretic acid 的检测 IC50 分别为 41.223 μM 和 45.646 μM[2]。 |
| In Vivo |
与对照组 ob/ob 饮食组相比，高剂量 Nordihydroguaiaretic acid (NDGA) 饮食组从 9 周开始体重显著下降，而从 12 周开始低剂量组。Nordihydroguaiaretic acid 处理导致 ob/ob 小鼠的体温 (直肠) 温度升高，尤其是在高剂量 Nordihydroguaiaretic acid[3]时。 |
| 细胞实验 |
MTT assay is used to measure cell growth-inhibitory activity of the selected most promising compounds in HepG2 cell lines. Cells are cultured in 96-well culture plate at 1×104 cells/well. After 24 h cultured at 37 °C in the atmosphere of 5% CO2， cells are adhered and treated with different concentrations of the targeted compounds (e.g.， Nordihydroguaiaretic acid， 0， 30， 60， 80， 100， 120， and 140 μM) and incubated for 24 h. Then， the supernatants are discarded and MTT (0.5 mg/mL) is added to each well and incubated at 37°C in 5% CO2 for an additional 4 h. Following， the MTT is removed and 150 μL of formazan in DMSO is added to terminate response and then plates are set to the table shaker for 5 min at low speed. Cell proliferation is evaluated by measuring the absorbance at 570 nm using ELISA Plate Reader. The IC50 values are calculated by SPSS statistics 17.0[2]. |
| 动物实验 |
Mice[3]Seven-week-old male control C57BL/6J mice， male leptin-deficient (ob/ob) mice， and male Pparα-deficient mutant mice (B6.129S4-Pparatm1Gonz/J) are used. These mice are fed a standard chow diet for 1 wk to allow them to acclimatize to a controlled new environment (25±2°C， 55±5% relative humidity with a 12-h light-dark cycle). Subsequently， one group of ob/ob mice is switched to a chow diet supplemented with either low- (0.83 g/kg chow diet) or high-dose (2.5 g/kg chow diet) Nordihydroguaiaretic acid and maintained on this diet for 16 wk. The other groups of ob/ob mice and control mice continue to be fed a normal chow diet for 16 wk. In another set of studies， C57BL/6J mice and Pparα-deficient mutant mice are fed either a high-fat diet (~60% of total calories come from fat)， or the same high-fat diet supplemented with a high dose of Nordihydroguaiaretic acid (2.5 g/kg diet). Food intake and body weights are measured once a week throughout the experiment. |
| 数据来源文献 |
[1]. West M， et al. The arachidonic acid 5-lipoxygenase inhibitor Nordihydroguaiaretic acid inhibits tumor necrosis factor alpha activation of microglia and extends survival of G93A-SOD1 transgenic mice. J Neurochem. 2004 Oct;91(1):133-43.
[2]. Lu F， et al. Virtual Screening for Potential Allosteric Inhibitors of Cyclin-Dependent Kinase 2 from Traditional Chinese Medicine. Molecules. 2016 Sep 21;21(9). pii: E1259.
[3]. Zhang H， et al. Nordihydroguaiaretic acid improves metabolic dysregulation and aberrant hepatic lipid metabolism in mice by both PPARα-dependent and -independent pathways. Am J Physiol Gastrointest Liver Physiol. 2013 Jan 1;304(1):G72-86. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
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