香胶甾酮

中文名称:

香胶甾酮

中文同义词:

咕咕草;香胶甾酮;木苦甾酮 (固甾酮);固甾酮(木苦甾酮);固甾酮;(17Z)-孕甾-4,17(20)-二烯-3,16-二酮;孕二烯二酮 标准品;固甾酮 香胶甾酮

英文名称:

(Z)-Guggulsterone

英文同义词:

4,17(20)-(CIS)-PREGNADIEN-3,16-DIONE;PREGNA-4,17(20)-DIENE-3,16-DIONE;(8S,9R,10R,13S,14S,17E)-17-(1-methoxyethylidene)-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15-decahydrocyclopenta[a]phenanthrene-3,16-dione;pregna-4,17-diene-3,16-dione;GUGGULISTERONES 95%;CIS-4,17(20)-PREGNADIENE-3,16-DIONE;CIS GUGGULSTERONE;GUGULSTERONE

CAS号:

95975-55-6

分子式:

C21H28O2

分子量:

312.45

EINECS号:

1308068-626-2

相关类别:

原料药;医药原料;医药类别;医药原料药;原料药;Miscellaneous

Mol文件:

95975-55-6.mol

沸点 

463.3±45.0 °C(Predicted)

密度 

1.10±0.1 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

DMSO: 5 mg/mL

形态

powder

颜色

light yellow

CAS 数据库

95975-55-6(CAS DataBase Reference)

生物活性

Guggulsterone 是一种植物甾醇，来自 Commiphora wightii 树的树胶脂。 Guggulsterone 通过下调抗细胞凋亡 (apoptosis) 基因产物 (IAP1，xIAP，Bfl-1/A1，Bcl-2，cFLIP，survivin)，调节细胞周期蛋白 (cyclin D1，c-Myc)，激活 caspases，JNK，抑制 Akt，抑制多种肿瘤细胞的生长并诱导细胞凋亡。Guggulsterone 通过调节几种转录因子介导基因表达，包括 NF-κB，STAT3，C /EBPα，雄激素受体 (androgen receptor) 和糖皮质激素受体(glucocorticoid receptors)。Guggulsterone，一种法尼醇 X 受体 (FXR) 拮抗剂，可降低 CDCA 诱导的 FXR 活化，Z- 和 E-Guggulsterone 的 IC50 分别为 17 和 15 μM。

靶点

JNK Akt Caspase

JNK

Akt

体外研究

Guggulsterone (0.5-20 μM; 24 hours) suppresses TREM-1, TLR4 and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS. Western Blot Analysis Cell Line: RAW 264.7 murine macrophage cells Concentration: 0.5, 5, 10, 20 μM Incubation Time: 24 hours Result: Suppressed TREM-1, TLR4, and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS.

Cell Line:

RAW 264.7 murine macrophage cells

Concentration:

0.5, 5, 10, 20 μM

Incubation Time:

24 hours

Result:

Suppressed TREM-1, TLR4, and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS.

体内研究

Guggulsterone (orally; 100 mg/kg once per day for 8 days) significantly improved the survival rates of wild-type mice with TNBS-induced colitis. Animal Model: Wild-type mice with TNBS-induced colitis Dosage: 100 mg/kg Administration: Orally; once per day; for 8 days Result: Improved the survival rates of wild-type mice with TNBS-induced colitis.

Animal Model:

Wild-type mice with TNBS-induced colitis

Dosage:

100 mg/kg

Administration:

Orally; once per day; for 8 days

Result:

Improved the survival rates of wild-type mice with TNBS-induced colitis.

危险品标志 

Xi

危险类别码 

37

安全说明 

36

WGK Germany 

3

海关编码 

29147000