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20(S)-原人参三醇

20(S)-原人参三醇用途

(20S)-Protopanaxatriol 是人参皂苷的代谢物,通过 glucocorticoid receptor 和 oestrogen receptor 起作用,同时为 LXRα 的抑制剂。

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20(S)-原人参三醇名称

[ CAS 号 ]:
34080-08-5

[ 中文名 ]:
原人参三醇

[ 英文名 ]:
(20S)-Protopanaxatriol

[中文别名 ]:

(S型)原人参三醇

[英文别名 ]:

PROTOPANAXTRIOL
20(S)-APPT,g-PPT
20S-Protopanaxatriol
Protopanaxatriol, 20S-
(20S)-Protopanaxatriol

20(S)-原人参三醇生物活性

[ 描述 ]:

(20S)-Protopanaxatriol 是人参皂苷的代谢物,通过 glucocorticoid receptor 和 oestrogen receptor 起作用,同时为 LXRα 的抑制剂。

[ 相关类别 ]:

信号通路 >> 其他 >> 雌激素受体/ERR

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 糖皮质激素受体

信号通路 >> 代谢酶/蛋白酶 >> LXR

研究领域 >> 心血管疾病

天然产物 >> 类固醇

[ 靶点 ]

Glucocorticoid receptor, Oestrogen receptor[1], LXRα[2]

[体外研究]

(20S)-Protopanaxatriol通过人脐静脉内皮细胞(HUVEC)中的糖皮质激素受体(GR)和雌激素受体(ER)起作用。 (20S)-Protopanaxatriol(g-PPT)在HUVEC中增加[Ca2 +] i,EC50为482nM。 (20S)-Protopanaxatriol(1μM)通过ERβ提高NO产生[1]。 (20S)-Protopanaxatriol(PPT)抑制Gal4-LXRαLBD的自主反式激活,这是T0901317依赖的SREBP-1c及其启动子的转录。 (20S)-Protopanaxatriol(10μg/ mL)阻断RNA聚合酶II向SREBP-1c的LXRE区域的募集。 (20S)-Protopanaxatriol还抑制与脂肪生成相关的LXRα靶基因的T0901317依赖性转录,并减少T0901317诱导的原代肝细胞中的细胞甘油三酯(TG)积累,但不改变ABCA1的转录,也是LXRα靶基因的转录[2] 。

[参考文献]

[1]. Leung KW, et al. Protopanaxadiol and protopanaxatriol bind to glucocorticoid and oestrogen receptors in endothelial cells. Br J Pharmacol. 2009 Feb;156(4):626-37.

[2]. Oh GS, et al. 20(S)-protopanaxatriol inhibits liver X receptor α-mediated expression of lipogenic genes in hepatocytes. J Pharmacol Sci. 2015 Jun;128(2):71-7.

[相关活性小分子]

20(S)-原人参三醇物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
588.8±50.0 °C at 760 mmHg

[ 分子式 ]:
C₃₀H₅₂O₄

[ 分子量 ]:
476.73

[ 闪点 ]:
242.9±24.7 °C

[ PSA ]:
80.92000

[ LogP ]:
5.41

[ 蒸汽压 ]:
0.0±3.7 mmHg at 25°C

[ 折射率 ]:
1.541

[ 储存条件 ]:
-20°C

20(S)-原人参三醇安全信息

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

20(S)-原人参三醇文献

Dual functions of ginsenosides in protecting human endothelial cells against influenza H9N2-induced inflammation and apoptosis.

J. Ethnopharmacol. 137 , 1542-1546, (2011)

Panax ginseng is a precious traditional Chinese herbal medicine which has been utilized as herbal tonic for improving immunity. The active component, ginsenosides have been shown to possess various ph...

Cytochrome P450 CYP716A53v2 catalyzes the formation of protopanaxatriol from protopanaxadiol during ginsenoside biosynthesis in Panax ginseng.

Plant Cell Physiol. 53 , 1535-1545, (2012)

Ginseng (Panax ginseng C.A. Meyer) is one of the most popular medicinal herbs, and the root of this plant contains pharmacologically active components, called ginsenosides. Ginsenosides, a class of te...

The in vitro structure-related anti-cancer activity of ginsenosides and their derivatives.

Molecules 16(12) , 10619-30, (2011)

Panax ginseng has long been used in Asia as a herbal medicine for the prevention and treatment of various diseases, including cancer. The current study evaluated the cytotoxic potency against a variet...

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