CAS:500-38-9
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥98%
Appearance:White to yellow Solid
是一种 5-脂氧合酶 (5LOX)和酪氨酸激酶抑制剂。
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Nordihydroguaiaretic AcidCAS:500-38-9
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥98%
Appearance:White to yellow Solid
CAS | 500-38-9 |
Chinese Name | 去甲二氢愈创木酸 |
English Name | Nordihydroguaiaretic Acid |
Synonyms | NDGA;Dihydronorguaiaretic Acid |
Molecular Formula | C18H22O4 |
Molecular Weight | 302.37 |
Solubility | Soluble in DMSO |
Purity | HPLC≥98% |
Appearance | White to yellow Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 207-903-0 |
MDL | MFCD00002206 |
SMILES | CC(CC1=CC=C(O)C(O)=C1)C(C)CC2=CC=C(O)C(O)=C2 |
InChIKey | HCZKYJDFEPMADG-UHFFFAOYSA-N |
InChI | InChI=1S/C18H22O4/c1-11(7-13-3-5-15(19)17(21)9-13)12(2)8-14-4-6-16(20)18(22)10-14/h3-6,9-12,19-22H,7-8H2,1-2H3 |
PubChem CID | 4534 |
Target Point | 5-Lipoxygenase |
Passage | Metabolic Enzyme&Protease |
Background | Nordihydroguaiaretic Acid is a 5-lipoxygenase (5LOX) and tyrosine kinase inhibitor. |
Biological Activity | Nordihydroguaiaretic acid 是一种 5-脂氧合酶 (5LOX) (IC50=8±3 μM) 和酪氨酸激酶抑制剂。[1-3] |
IC50 | 8±3μM(5LOX)[1] |
In Vitro | 天然的二儿茶酚二氢愈创木酸(NDGA)是来自杂酚油植物(Larrea tridentata:Zygophyllaceae)的选择性5LOX抑制剂。抑制5LOX的天然二儿茶酚去甲二氢愈创木酸是TNFα刺激的小胶质细胞激活的非常有效的无毒拮抗剂。 Nordihydhydroguaiaretic acid的体外效力约为米诺环素的6倍,IC50值为8±3μM,100μM时无毒性。在800nM的去甲二氢愈创木酸中观察到显著的NO 2 - 抑制。对于天然和合成的去甲二氢愈创木酸以及去甲二氢愈创木酸的乙酰酯,观察到类似的功效。 Nordihydhydroguaiaretic acid还抑制TNFα刺激的EOC-20细胞产生PGE2,IC50为841 nM [1]。为了测试前列腺素E1和去甲二氢愈创木酸(NDGA)对癌细胞系的增殖作用,HepG2细胞系用各种方法治疗。通过MTT测定检查两种化合物和阳性化合物8-苯胺基-1-萘磺酸盐(ANS)的剂量,持续24小时和细胞活力。 ANS显示剂量依赖性抑制(0,10,30,50,100,100,120和150μM),估计的IC 50为25.888μM。在0,30,60,80,100,120和140μM的不同浓度下,前列腺素E1的测试IC50分别为41.223μM和去甲二氢愈创木酸为45.646μM[2]。 |
In Vivo | 与对照ob/ob食物组相比,在高剂量去甲二氢愈创木酸(NDGA)饮食组中从9周处理开始,并且在低剂量组中从12周开始,体重显著降低。 Nordihydhyduauaiaretic acid治疗导致ob/ob小鼠的体温(直肠)温度升高,尤其是高剂量的Nordihydroguaiaretic acid [3]。 |
Cell Experiment | MTT测定用于测量HepG2细胞系中所选择的最有希望的化合物的细胞生长抑制活性。将细胞以1×10 4个细胞/孔在96孔培养板中培养。在37℃,5%CO 2气氛中培养24小时后,将细胞粘附并用不同浓度的目标化合物(例如,去甲二氢愈创木酸,0,30,60,80,100,120和140μM)处理。并孵育24小时。然后,弃去上清液并向每个孔中加入MTT(0.5mg/mL)并在37℃,5%CO 2中再孵育4小时。然后,除去MTT并加入150μL甲硫酸的DMSO终止反应,然后将板在低速下放置在台式振荡器中5分钟。通过使用ELISA Plate Reader测量570nm处的吸光度来评估细胞增殖。 IC50值由SPSS统计17.0 [2]计算。 |
Animal Experiment | 小鼠[3]使用7周龄雄性对照C57BL/6J小鼠,雄性瘦蛋白缺陷型(ob/ob)小鼠和雄性Pparα缺陷型突变小鼠(B6.129S4-Pparatm1Gonz/J)。给这些小鼠喂食标准食物饲料1周,使它们适应受控的新环境(25±2℃,55±5%相对湿度,12小时光暗循环)。随后,将一组ob/ob小鼠改为补充低 -(0.83g/kg食物饮食)或高剂量(2.5g/kg食物饮食)去甲二氢愈创木酸的食物,并在该饮食中维持16周。其他组的ob/ob小鼠和对照小鼠继续喂食正常的饲料,持续16周。在另一组研究中,C57BL/6J小鼠和Pparα缺陷型突变小鼠喂食高脂肪饮食(约占总热量的60%来自脂肪),或同样的高脂肪饮食补充高剂量的Nordihydroguauaretic酸(2.5克/千克饮食)。在整个实验过程中每周测量一次食物摄取和体重。 |
Data Literature Source | [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. |
Unit | Bottle |
Specification | 10mg 10mM*1mL in DMSO 20mg |
是一种 5-脂氧合酶 (5LOX)和酪氨酸激酶抑制剂。