甲氧醉椒素

中文名称:

甲氧醉椒素

中文同义词:

甲氧醉椒素, 来源于卡瓦胡椒;甲氧醉椒素、麻醉椒素;卡法椒素;甲氧醉椒素;麻醉椒素,甲氧醉椒素;4-甲氧基-6-[(E)-2-(4-甲氧基苯基)乙烯基]-2H-吡喃-2-酮;甲氧基醉椒素

英文名称:

YANGONIN

英文同义词:

YANGONIN;11-METHOXYYANGONIN;4-methoxy-6-(beta-(p-anisyl)vinyl)-alpha-pyrone;4-methoxy-6-(p-methoxystyryl)-2h-pyran-2-on;4-methoxy-6-(p-methoxystyryl)-2h-pyran-2-one;5-hydroxy-3-methoxy-7-(p-methoxyphenyl)-2,4,6-heptatrienoicacidgamma-lacton;4-Methoxy-6-[2-(4-methoxyphenyl)ethenyl]-2H-pyran-2-one;4-Methoxy-6-[(E)-2-(4-methoxyphenyl)vinyl]-2H-pyran-2-one

CAS号:

500-62-9

分子式:

C15H14O4

分子量:

258.27

EINECS号:

相关类别:

对照品;中药对照品;标准品;植物提取物;标准品-对照品;标准品 -中药标准品;标准品，对照品;Aromatics;Heterocycles;Mutagenesis Research Chemicals

Mol文件:

500-62-9.mol

熔点 

155-157°

沸点 

487.6±45.0 °C(Predicted)

密度 

1.325 g/cm3

储存条件 

2-8°C

形态

neat

BRN 

230710

用途

甲氧醉椒素是从卡瓦植物(Piper methysticum)中分离的内酯。卡瓦的活性成分是一组约。18种化合物统称为卡瓦内酯或卡瓦吡酮。卡瓦内酯、二氢卡瓦内酯、甲基卡瓦内酯、二氢甲基卡瓦内酯、甲氧醉椒素和去甲氧基醉椒素是6种主要的卡瓦内酯。卡瓦饮料和其他制剂被认为是抗焦虑的，用于治疗焦虑症。含有卡瓦灌木根的膳食补充剂已经涉及到几个人的肝脏毒性案例，包括几个在使用卡瓦补充剂后需要肝脏移植的人。

生物活性

Yangonin 对人重组大麻素 CB1 受体具有高的亲和力，IC50 和 Ki 分别为 1.79 μM 和 0.72 μM。

靶点

CB1 1.79 μM (IC 50 ) CB1 0.72 μM (Ki) RelA

CB1 1.79 μM (IC 50 )

CB1 0.72 μM (Ki)

体外研究

Yangonin is one of the six major kavalactones found in Piper methysticum .Yangonin potently inhibits NF-κB activation through suppression of the transcriptional activity of the RelA/p65 subunit of NF-κB. Yangonin significantly inhibits the induced expression of the NF-κB-reporter gene. However, Yangonin does not interfere with TNF-α-induced inhibitor of κBα (IκBα) degradation, p65 nuclear translocation, and DNA-binding activity of NF-κB. Yangonin inhibits not only the induced NF-κB activation by overexpression of RelA/p65, but also transactivation activity of RelA/p65. Yangonin does not inhibit TNF-α-induced activation of p38, but it significantly impairs activation of ERK 1/2 and stress-activated protein kinase/JNK.

化学性质 

可溶于甲醇、乙醇、DMSO等有机溶剂，来源于卡瓦胡椒Piper methysticum Forst根。

用途 

抑制呼吸道平滑肌收缩，抗关节炎，平喘。

用途 

用于含量测定/鉴定/药理实验等

WGK Germany 

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