Azuleno[6,5-b]furan-2,5-dione,4-(acetyloxy)-3,3a,4,4a,7a,8,9,9a-octahydro-4a,8-dimethyl-3-methylene-,(3aR,4S,4aR,7aR,8R,9aR)

• 常用名: Azuleno[6,5-b]furan-2,5-dione,4-(acetyloxy)-3,3a,4,4a,7a,8,9,9a-octahydro-4a,8-dimethyl-3-methylene-,(3aR,4S,4aR,7aR,8R,9aR)
• 英文名: Azuleno[6,5-b]furan-2,5-dione,4-(acetyloxy)-3,3a,4,4a,7a,8,9,9a-octahydro-4a,8-dimethyl-3-methylene-,(3aR,4S,4aR,7aR,8R,9aR)
• CAS号: 10180-86-6
• 分子量: 304.33800
• 密度: 1.22g/cm3
• 沸点: 466.6ºC at 760 mmHg
• 分子式: C₁₇H₂₀O₅
• 熔点: N/A
• 闪点: 207.1ºC

用途

Helenalin acetate是一种天然的NF-κB抑制剂,是一种有效的C/EBPβ抑制剂。Helenalin醋酸盐具有抗炎和抗癌活性[1]。

名称

• 英文名: [(3aR,5R,5aR,8aR,9S,9aR)-5,8a-dimethyl-1-methylidene-2,8-dioxo-3a,4,5,5a,9,9a-hexahydroazuleno[6,5-b]furan-9-yl] acetate

生物活性

• 描述: Helenalin acetate是一种天然的NF-κB抑制剂,是一种有效的C/EBPβ抑制剂。Helenalin醋酸盐具有抗炎和抗癌活性[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 表观遗传学 >> 组蛋白去甲基化酶
  研究领域 >> 炎症/免疫
• 体外研究: Helenalin醋酸盐(0.1-1μM持续 7.天)显着抑制 3吨-1细胞的分化[1]。 Helenalin醋酸盐对急性髓性白血病细胞具有抗增殖作用,对正常造血祖细胞无作用[1]。 Helenalin醋酸盐通过结合到 C/EBPβ的 N末端部分来抑制 C/EBPβ从而破坏 C/EBPβ与共激活因子 第300页的合作。Helenalin醋酸盐仅选择性抑制全长(富含肝脏的激活蛋白* (圈*))同种型,但不抑制稍短的 (圈)同种型[1]。 细胞分化试验[1]细胞系：3T3-L1细胞浓度：0.1μM、0.3μM、1μM培养时间：7天结果：显著抑制分化。
• 参考文献:

  [1]. Jakobs A, et al. Helenalin Acetate, a Natural Sesquiterpene Lactone with Anti-inflammatory and Anti-cancer Activity, Disrupts the Cooperation of CCAAT Box/Enhancer-binding Protein β (C/EBPβ) and Co-activator p300. J Biol Chem. 2016 Dec 9;291(50):26098-26108.

物理化学性质

• 密度: 1.22g/cm3
• 沸点: 466.6ºC at 760 mmHg
• 分子式: C₁₇H₂₀O₅
• 分子量: 304.33800
• 闪点: 207.1ºC
• 精确质量: 304.13100
• PSA: 69.67000
• LogP: 1.81710
• InChIKey: DCNRYQODUSSOKC-HKHYKUHTSA-N
• SMILES: C=C1C(=O)OC2CC(C)C3C=CC(=O)C3(C)C(OC(C)=O)C12
• 蒸汽压: 6.95E-09mmHg at 25°C
• 折射率: 1.541

靶点实验

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英文别名

• 6-O-acetylhelenalin
• Helenalin acetate
• Helenalin 6-acetate
• Angustibalin
• HELANIN ACETATE
• O-Acetyl-helenalin
• acetylhelenalin