雷公藤内酯酮
| 中文名称 | 雷公藤内酯酮 |
|---|---|
| 中文同义词 | 雷公藤内酯酮(雷藤酮 ,雷公藤羰内酯);雷公藤内酯酮(标准品);雷藤酮 ,雷公藤羰内酯;雷藤酮;雷公藤内酯酮;雷公藤羰内酯;雷公藤内酯酮, 来源于前胡;雷公藤内酯酮(雷藤酮 |
| 英文名称 | Triptonide |
| 英文同义词 | TRIPTONIDE;TRIPTONIDE(PRIMARY STANDARD);NSC 165677;PG 492;(3bS,4aS,5aS,6aS,7aS,7bS,8aS,8bS)-6a-Isopropyl-8b-methyl-3b,4,4a,7a,7b,8b,9,10-octahydrotrisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1,6(3H,6aH)-dione;14-Deoxy-14-oxotriptolide;Triptolide,14-deoxy-14-oxo;Triptonide, 98%, from Peucedanum praeruptorum Dunn |
| CAS号 | 38647-11-9 |
| 分子式 | C20H22O6 |
| 分子量 | 358.39 |
| EINECS号 | |
| 相关类别 | 天然产物;植提标准品;中药对照品;标准品;植物提取物;对照品;中草药成分;标准品-中药标准品;Heterocycles;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract;新品;标准品 -中药标准品;标准品，对照品 |
| Mol文件 | 38647-11-9.mol |
| 结构式 |  |
雷公藤内酯酮 性质
| 熔点 | 251～252℃ |
|---|---|
| 沸点 | 581.1±50.0 °C(Predicted) |
| 密度 | 1.48±0.1 g/cm3(Predicted) |
| 储存条件 | Inert atmosphere,Store in freezer, under -20°C |
| 溶解度 | 二氯甲烷（微溶）、甲醇（微溶） |
| 形态 | 固体 |
| 颜色 | 灰白色至浅米色 |
| Target | Value |
|
Wnt/β-catenin
() |
Triptonide blocks Wnt/β-catenin signaling via C-terminal transactivation domain of β-catenin, and promots apoptosis in Wnt-dependent cancer cells.
Triptonide potently inhibits the proliferation of human B-lymphoma Raji and T-lymphoma Jurkat cells with IC
50
of 5.7 nM and 4.8 nM, respectively.
Triptonide (2.5-10 nM; 6 days) significantly suppresses B-lymphoma cell colony-forming capability.
Triptonide (20 nM; 3 days) promotes apoptosis through activation of PARP and caspase 3, but reduction of BCL2 protein levels in the lymphoma cells.
Triptonide (5-10 nM; 72 hours) markedly reduces both total and phosphorylated Lyn proteins, and diminishes Lyn downstream ERK and ATK signal pathways.
Cell Proliferation Assay
| Cell Line: | B-lymphoma Raji cells, T-lymphoma Jurkat cells |
| Concentration: | 0-80 nM |
| Incubation Time: | 3 days, 6 days |
| Result: | Inhibited lymphoma cell tumorigenic capability in a dose-dependent manner. |
Apoptosis Analysis
| Cell Line: | Raji cells |
| Concentration: | 5 nM, 10 nM, 20 nM |
| Incubation Time: | 3 days |
| Result: | Did not significantly induce apoptosis at the effective tumor growth-inhibitory (2.5-10 nM); moderately induced lymphoma cell apoptosis (20 nM). |
Western Blot Analysis
| Cell Line: | Raji cells |
| Concentration: | 5 nM, 10 nM, 20 nM |
| Incubation Time: | 3 days |
| Result: | Did not vigorously activated pro-apoptotic proteins PARP and caspase 3 in lymphoma cells (5-10 nM); significantly activated PARP and caspase 3 (20 nM); significantly reduced anti-apoptotic BCL2 levels. |
RT-PCR
| Cell Line: | Raji cells |
| Concentration: | 5 nM, 10 nM |
| Incubation Time: | 72 hours |
| Result: | Significantly diminished Lyn mRNA levels in the lymphoma cells. |
Triptonide (5 mg/kg; i.p.; daily; for 34 days) exerts a strong anti-lymphoma effect in mice.
| Animal Model: | Eight-week-old female NOD/SCID mice (18-22 g), with 3 x 10 7 Raji cells xenograft |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection, daily, for 34 days |
| Result: | Potently inhibited lymphoma cell growth and tumorigenic capability. |
药理药效:治疗麻风反应,治疗类风湿性关节炎,治疗肺结核及其他慢性肺部疾病。
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-32736 | Triptonide | 5 mg | 1278元 | |
| 2024/01/25 | HY-32736 | 雷公藤内酯酮 Triptonide | 38647-11-9 | 10mg | 2046元 |