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缬草素

缬草素用途

缬草酸((-)-缬草酸)是一种倍半萜类化合物,是GABAA受体的口服活性阳性变构调节剂。缬草酸也是5-HT5a受体的部分激动剂。缬草酸通过含有β3亚单位的GABAA受体介导抗焦虑活性。缬草酸还具有强大的抗氧化性能[1][2][3]。

缬草素名称

[ CAS 号 ]:
3569-10-6

[ 中文名 ]:
缬草烯酸

[ 英文名 ]:
Valerenic acid

[中文别名 ]:

缬草素

[英文别名 ]:

MFCD00075694
7-Hydroxy-PIPAT maleate
Valerenic acid

缬草素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

5-HT5A Receptor:17.2 μM (IC50)

GABAA

[体外研究]

缬草酸(1-100μM)增强HEK 293细胞中表达的GABAA受体的全细胞电流[1]。缬草酸对5-HT5a受体具有显著的亲和力,IC50为17.2μM(Ki=10.7μM)[2][3H]缬草酸与脑膜结合,显示出高亲和力结合位点(KD=25 nM)和低亲和力位点(KD=16μM)[1][3H]缬草酸被高效的缬烯醇取代(IC50=3 nM)[1]。

[体内研究]

缬草酸(1-6 mg/kg i.p.或10 mg/kg p.o.)可降低野生型小鼠对照明区域的厌恶[2]。缬草酸(10mg/kg；p、 o.)增加129X1/SvJ小鼠伸开双臂的时间比例[2]。

[参考文献]

[1]. Benke D, et, al. GABA A receptors as in vivo substrate for the anxiolytic action of valerenic acid, a major constituent of valerian root extracts. Neuropharmacology. 2009 Jan;56(1):174-81.

[2]. Dietz BM, et, al. Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro. Brain Res Mol Brain Res. 2005 Aug 18;138(2):191-7.

[3]. Kara M, et, al. Ameliorative Effects of the Sesquiterpenoid Valerenic Acid on Oxidative Stress Induced in HepG2 Cells after Exposure to the Fungicide Benomyl. Antioxidants (Basel). 2021 May 8;10(5):746.

[4]. Becker A, et, al. The anxiolytic effects of a Valerian extract is based on valerenic acid. BMC Complement Altern Med. 2014 Jul 28;14:267.

缬草素物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
374.5±21.0 °C at 760 mmHg

[ 熔点 ]:
134-139ºC

[ 分子式 ]:
C₁₅H₂₂O₂

[ 分子量 ]:
234.334

[ 闪点 ]:
274.2±13.0 °C

[ 精确质量 ]:
234.161987

[ PSA ]:
37.30000

[ LogP ]:
5.13

[ 外观性状 ]:
棕色-黄色粉末

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.529

[ 储存条件 ]:
−20°C

缬草素MSDS

缬草素安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ WGK德国 ]:
3

缬草素合成路线

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缬草素文献

Concise synthesis of Valerena-4,7(11)-diene, a highly active sedative, from valerenic acid.

Biosci. Biotechnol. Biochem. 74(9) , 1963-4, (2010)

A concise synthesis of valerena-4,7(11)-diene with potent sedative activity was achieved in three steps involving, reduction of carboxylic acid, bromination of the resulting alcohol, and reduction of ...

Root colonization by symbiotic arbuscular mycorrhizal fungi increases sesquiterpenic acid concentrations in Valeriana officinalis L.

Planta Med. 76(4) , 393-8, (2010)

In some medicinal plants a specific plant-fungus association, known as arbuscular mycorrhizal (AM) symbiosis, increases the levels of secondary plant metabolites and/or plant growth. In this study, th...

Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro.

Brain Res. Mol. Brain Res. 138(2) , 191-7, (2005)

Insomnia is the most frequently encountered sleep complaint worldwide. While many prescription drugs are used to treat insomnia, extracts of valerian (Valeriana officinalis L., Valerianaceae) are also...

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缬草素