Triptonide (NSC 165677) 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、避育、神经保护和抗淋巴瘤作用。
| 生物活性 | Triptonide (NSC 165677) is a natural product identified inTripterygium wilfordiiHook F.. Triptonide is aWntsignaling inhibitor with anIC50of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects[1][2]. |
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体外研究
(In Vitro) | Triptonide blocks Wnt/β-catenin signaling via C-terminal transactivation domain of β-catenin, and promots apoptosis in Wnt-dependent cancer cells[1].
Triptonide potently inhibits the proliferation of human B-lymphoma Raji and T-lymphoma Jurkat cells with IC50of 5.7 nM and 4.8 nM, respectively[2].
Triptonide (2.5-10 nM; 6 days) significantly suppresses B-lymphoma cell colony-forming capability[2].
Triptonide (20 nM; 3 days) promotes apoptosis through activation of PARP and caspase 3, but reduction of BCL2 protein levels in the lymphoma cells[2].
Triptonide (5-10 nM; 72 hours) markedly reduces both total and phosphorylated Lyn proteins, and diminishes Lyn downstream ERK and ATK signal pathways[2].
Cell Proliferation Assay[2] | 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[2] | 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[2] | 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[2] | Cell Line: | Raji cells | | Concentration: | 5 nM, 10 nM | | Incubation Time: | 72 hours | | Result: | Significantly diminished Lyn mRNA levels in the lymphoma cells. |
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体内研究
(In Vivo) | Triptonide (5 mg/kg; i.p.; daily; for 34 days) exerts a strong anti-lymphoma effect in mice[2].
| Animal Model: | Eight-week-old female NOD/SCID mice (18-22 g), with 3 x 107Raji cells xenograft[2] | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection, daily, for 34 days | | Result: | Potently inhibited lymphoma cell growth and tumorigenic capability. |
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| 来源 | - Plants
- Celastraceae
- Tripterygium wilfordiiHook. f.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(279.03 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7903 mL | 13.9513 mL | 27.9026 mL | | 5 mM | 0.5581 mL | 2.7903 mL | 5.5805 mL | | 10 mM | 0.2790 mL | 1.3951 mL | 2.7903 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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