中文名 | 雷公藤内酯酮 |
英文名 | Triptonide |
别名 | 雷藤酮 雷公藤内酯酮 雷公藤羰内酯 雷公藤内酯酮(雷藤酮 雷藤酮 ,雷公藤羰内酯 雷公藤内酯酮(标准品) 雷公藤内酯酮, 来源于前胡 雷公藤内酯酮(雷藤酮 ,雷公藤羰内酯) |
英文别名 | PG 492 Triptonide TRIPTONIDE troptonide NSC 165677 14-Deoxy-14-oxotriptolide Triptolide,14-deoxy-14-oxo TRIPTONIDE(PRIMARY STANDARD) Triptolide, 14-deoxy-14-oxo- |
CAS | 38647-11-9 |
化学式 | C20H22O6 |
分子量 | 358.39 |
InChI | InChI=1/C20H22O6/c1-8(2)18-13(25-18)14-20(26-14)17(3)5-4-9-10(7-23-15(9)21)11(17)6-12-19(20,24-12)16(18)22/h8,11-14H,4-7H2,1-3H3/t11-,12-,13-,14-,17-,18-,19+,20+/m0/s1 |
密度 | 1.48±0.1 g/cm3(Predicted) |
熔点 | 251~252℃ |
沸点 | 581.1±50.0 °C(Predicted) |
比旋光度 | -175°(C=0.148,chloroform) |
闪点 | 257.8°C |
蒸汽压 | 1.7E-13mmHg at 25°C |
溶解度 | 二氯甲烷 (微溶) 、甲醇 (微溶) |
折射率 | 1.637 |
存储条件 | Inert atmosphere,Store in freezer, under -20°C |
外观 | 固体 |
颜色 | Off-White to Pale Beige |
物化性质 | 黄色结晶粉末,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于雷公藤。 |
MDL号 | MFCD00210566 |
体外研究 | 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. |
体内研究 | 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. |
参考资料 展开查看 | 1. Liu, Xiufeng, et al. "Computational prediction and experimental validation of low-affinity target of triptolide and its analogues." RSC advances 5.44 (2015): 34572-34579.DOI https://doi.org/10.1039/C4RA17009A 2. [IF=3.361] Xiufeng Liu et al."Computational prediction and experimental validation of low-affinity target of triptolide and its analogues."Rsc Adv. 2015 Apr;5(44):34572-34579 |