固甾酮

固甾酮用途

Z-guggulsterone 是印度阿育吠陀药用植物 Commiphora mukul 的成分,通过引起细胞凋亡 (apoptosis) 来抑制人前列腺癌细胞的生长。 Z-guggulsterone 通过抑制 VEGF-VEGF-R2-Akt 信号传导轴来抑制血管生成。

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固甾酮名称

[ CAS 号 ]:
39025-23-5

[ 中文名 ]:
孕二烯二酮

[ 英文名 ]:
Z-Guggulsterone

[中文别名 ]:

[英文别名 ]:

Guggulsterone
(17E)-Pregna-4,17-diene-3,16-dione
UNII:9B259YE66O
Pregna-4,17(20)-diene-3,16-dione, (17E)-
(17E)-Pregna-4,17(20)-diene-3,16-dione
E-guggulsterone
Pregna-4,17-diene-3,16-dione, (17E)-
trans-Guggulsterone
GUGGULSTERONE, (E)-

固甾酮生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> PI3K/Akt/mTOR 信号通路 >> AKT

信号通路 >> 蛋白酪氨酸激酶 >> VEGFR

[ 靶点 ]

VEGF-R2

Akt

[体外研究]

Z-guggulsterone(10,20μM; 24或48小时)导致HUVEC中VEGF-R2蛋白水平降低[1]。Western Blot分析[1]细胞系：血管内皮生长因子(VEGF)浓度：10,20μM孵育时间：24或48小时结果：导致HUVEC中VEGF-R2蛋白水平降低。

[体内研究]

Z-guggulsterone(口服；1mg；5次/周)导致肿瘤体积和湿肿瘤重量的统计学显着降低[1]。动物模型：雄性裸鼠(5-6周龄)s.c.植入含DU145细胞的Matrigel塞剂量：1mg给药：口服；5次/周结果：导致肿瘤体积和湿肿瘤重量的统计学显着降低。

[参考文献]

[1]. Xiao D, et al. z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Mol Cancer Ther. 2008 Jan;7(1):171-80.

固甾酮物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
463.3±45.0 °C at 760 mmHg

[ 熔点 ]:
188-190°

[ 分子式 ]:
C₂₁H₂₈O₂

[ 分子量 ]:
312.446

[ 闪点 ]:
172.3±25.7 °C

[ 精确质量 ]:
312.208923

[ PSA ]:
34.14000

[ LogP ]:
3.65

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.557

[ 储存条件 ]:
2-8°C

固甾酮MSDS

详细MSDS(安全技术说明书)

固甾酮安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R37

[ 安全声明 (欧洲) ]:
S36

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

[ WGK德国 ]:
3

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固甾酮文献

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Nat. Chem. Biol. 5 , 765-71, (2009)

Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened...

Conformational dynamics of human FXR-LBD ligand interactions studied by hydrogen/deuterium exchange mass spectrometry: insights into the antagonism of the hypolipidemic agent Z-guggulsterone.

Biochim. Biophys. Acta 1844(9) , 1684-93, (2014)

Farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily of transcription factors that plays a key role in the regulation of bile acids, lipid and glucose metabolisms. The regulative...

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固甾酮