雷公藤内酯酮

概述生物活性靶点体外研究体内研究雷公藤内酯酮试剂级价格

雷公藤内酯酮

CAS号:38647-11-9
英文名:Triptonide
中文名:雷公藤内酯酮
CBNumber:CB0205245
分子式:C20H22O6
分子量:358.39
MOL File:38647-11-9.mol

雷公藤内酯酮化学性质

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 :Dichloromethane (Slightly), Methanol (Slightly)
形态 :Solid
颜色 :Off-White to Pale Beige

雷公藤内酯酮性质、用途与生产工艺

概述雷公藤内酯酮是从雷公藤中分离得到的一个二萜类化合物，是雷公藤的有效成份之一，它与雷公藤内酯醇结构相似，活性也相当，其结构式如下。雷公藤内酯酮具有抗雄性生育作用和对免疫功能具有一定的影响。
生物活性 Triptonide (NSC 165677;PG 492) 是从雷公藤中鉴定出的一种天然产物。Triptonide 是一种 Wnt 信号抑制剂，其 IC50 约为 0.3 nM。Triptonide 具有免疫抑制、抗炎、抗生育、神经保护和抗淋巴瘤作用。
靶点
Target Value
Wnt/β-catenin
()

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.