| 中文名称 | 香胶甾酮 |
| 英文名称 | (Z)-Guggulsterone |
| CAS号 | 95975-55-6 |
| 分子式 | C21H28O2 |
| 分子量 | 312.45 |
| EINECS号 | 1308068-626-2 |
| 沸点 | 463.3±45.0 °C(Predicted) |
| 密度 | 1.10±0.1 g/cm3(Predicted) |
| 溶解度 | 在DMSO中的溶解度为5 毫克/毫升 |
| 形态 | 粉末 |
| 颜色 | 浅黄色 |
| 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 |
香胶甾酮是一种植物甾醇,来自 Commiphora wightii 树的树胶脂。 香胶甾酮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。香胶甾酮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)。它是一种法尼醇 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。
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JNK
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Akt
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Caspase
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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. |
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. |