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甲氧醉椒素

甲氧醉椒素用途

Yangonin 对人重组大麻素 CB1 受体具有高的亲和力，IC₅₀ 和 K_i 分别为 1.79±0.53 μM 和 0.72±0.21 μM。

甲氧醉椒素名称

[ CAS 号 ]:
500-62-9

[ 中文名 ]:
甲氧醉椒素

[ 英文名 ]:
Yangonin

[中文别名 ]:

[英文别名 ]:

4-Methoxy-6-((E)-4-methoxystyryl)pyran-2-one
4-Methoxy-6-[b-(p-anisyl)vinyl]-a-pyrone
6-(p-Methoxystyryl)-4-methoxy-a-pyrone
Yangonin

甲氧醉椒素生物活性

[ 描述 ]:

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±0.53 μM 和 0.72±0.21 μM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 大麻素受体

研究领域 >> 炎症/免疫

天然产物 >> 其他

[ 靶点 ]

CB1 Receptor:1.79 μM (IC50)

CB1 Receptor:0.72 μM (Ki)

RelA

[体外研究]

Yangonin是Piper methysticum中发现的六种主要的kavalactones之一.Yangonin通过抑制NF-κB的RelA/p65亚基的转录活性,有效抑制NF-κB的活化。仰光素显着抑制NF-κB-报告基因的诱导表达。然而,仰光素不干扰TNF-α诱导的κBα(IκBα)降解抑制因子,p65核转位和NF-κB的DNA结合活性。仰光素不仅抑制RelA/p65过表达诱导的NF-κB活化,还抑制RelA/p65的反式激活活性。仰光素不抑制TNF-α诱导的p38活化,但它显着损害ERK 1/2和应激激活的蛋白激酶/ JNK的激活[2]。

[细胞实验]

将HeLa细胞以1×10 5个细胞/ mL接种在含有100μL含10％FBS的DMEM培养基的96孔板中并孵育过夜。将Yangonin溶解在DMSO中，并将DMSO加入所有平板中以补偿相同体积的DMSO。 24小时后，用不同浓度的仰光（0.1-3μM）预处理细胞1小时，然后用或不用TNF-α刺激24小时。随后，将细胞与MTT溶液（5mg / mL）一起培养3小时。活细胞将MTT转化为甲，在溶解于150μLDMSO后产生蓝紫色。通过ELISA板读数器测量570nm处的吸光度[2]。

[参考文献]

[1]. Ligresti A, et al. Kavalactones and the endocannabinoid system: the plant-derived yangonin is a novel CB₁ receptor ligand. Pharmacol Res. 2012 Aug;66(2):163-9.

[2]. Ma J, et al. Yangonin blocks tumor necrosis factor-α-induced nuclear factor-κB-dependent transcription by inhibiting the transactivation potential of the RelA/p65 subunit. J Pharmacol Sci. 2012;118(4):447-54.

[3]. Wruck CJ, et al. Kavalactones protect neural cells against amyloid beta peptide-induced neurotoxicity via extracellular signal-regulated kinase 1/2-dependent nuclear factor erythroid 2-related factor 2 activation. Mol Pharmacol. 2008 Jun;73(6):1785-95.

[相关活性小分子]

甲氧醉椒素物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
487.6±45.0 °C at 760 mmHg

[ 熔点 ]:
155-157ºC

[ 分子式 ]:
C₁₅H₁₄O₄

[ 分子量 ]:
258.269

[ 闪点 ]:
219.7±28.8 °C

[ 精确质量 ]:
258.089203

[ PSA ]:
48.67000

[ LogP ]:
1.75

[ 外观性状 ]:
淡黄色粉末

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.578

[ 储存条件 ]:
2-8°C

甲氧醉椒素MSDS

详细MSDS(安全技术说明书)

甲氧醉椒素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ1225200

CHEMICAL NAME :: 2H-Pyran-2-one, 4-methoxy-6-(p-methoxystyryl)-

CAS REGISTRY NUMBER :: 500-62-9

LAST UPDATED :: 199109

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C15-H14-O4

MOLECULAR WEIGHT :: 258.29

WISWESSER LINE NOTATION :: T6OVJ DO1 F1U1R DO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 177,261,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 177,261,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 41 mg/kg

TOXIC EFFECTS :: Behavioral - anticonvulsant

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 177,261,1969

甲氧醉椒素安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2932999099

甲氧醉椒素上下游产品

甲氧醉椒素上游产品

甲氧醉椒素下游产品

甲氧醉椒素海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

甲氧醉椒素文献

Fatal kavalactone intoxication by suicidal intravenous injection.

Forensic Sci. Int. 249 , e7-11, (2015)

Kavalactones are a group of compounds found in kava, a beverage or extract prepared from the rhizome of the kava plant (Piper methysticum). Traditionally kava extracts have been used for their anxioly...

Interaction of various Piper methysticum cultivars with CNS receptors in vitro.

Planta Med. 67(4) , 306-11, (2001)

Methanolic leaf and root extracts of the Hawaiian kava (Piper methysticum Forst.) cultivars, Mahakea, Nene, Purple Moi and PNG, were tested on binding affinities to CNS receptors including GABAA (GABA...

Kavalactones fail to inhibit alcohol dehydrogenase in vitro.

Phytomedicine 13(3) , 192-5, (2006)

In recent years, Kava kava (Piper methysticum, Forst. f., Piperaceae), a folkloric beverage and popular herbal remedy, has been implicated in a number of liver failure cases. Many hypotheses as to the...

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