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
- 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。
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靶点
Target Value Wnt/β-catenin
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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. - 化学性质 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。
- 用途 雷公藤内酯酮具有抗肿瘤 免疫调节 抗炎的作用。
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用途
用于含量测定/鉴定/药理实验等。
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。
- 更新日期：2024/11/11
- 产品编号：XW3864711901
- 产品名称：雷公藤内酯酮
- CAS编号：38647-11-9
- 包装：5MG
- 价格：380元
- 更新日期：2024/11/08
- 产品编号：HY-32736
- 产品名称：Triptonide
- CAS编号：
- 包装：5 mg
- 价格：1278元
- 公司名称：Pharma Affiliates
- 联系电话：--
- 电子邮件：@pharmaffiliates.com
- 国家：印度
- 产品数：6754
- 优势度：58
- 公司名称：Pharmaffiliates Analytics and Synthetics P. Ltd
- 联系电话：--
- 电子邮件：mktg@pharmaffiliates.com
- 国家：印度
- 产品数：6739
- 优势度：58
- 公司名称：CLEARSYNTH LABS LTD.
- 联系电话：--
- 电子邮件：sales@clearsynth.com
- 国家：印度
- 产品数：6257
- 优势度：58
