38647-11-9
38647-11-9 结构式
基本信息
雷公藤羰内酯
雷公藤内酯酮
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TRIPTONIDE
雷公藤内酯酮(雷藤酮 ,雷公藤羰内酯)
NSC 165677
TRIPTONIDE
Triptonide USP/EP/BP
14-Deoxy-14-oxotriptolide
Triptolide,14-deoxy-14-oxo
TRIPTONIDE(PRIMARY STANDARD)
Triptonide, 98%, from Peucedanum praeruptorum Dunn
(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
Trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1,6(3H,6aH)-dione, 3b,4,4a,7a,7b,8b,9,10-octahydro-8b-methyl-6a-(1-methylethyl)-, (3bS,4aS,5aS,6aS,7aS,7bS,8aS,8bS)-
物理化学性质
常见问题列表
| 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. |