| CAS |
No.38748-32-2 |
| 中文名称 |
雷公藤甲素(10mM in DMSO,无菌） |
| 英文名称 |
Triptolide(10mM in DMSO，Sterile） |
| 分子式 |
C20H24O6 |
| 分子量 |
360.4 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
NF-κB |
| 通路 |
NF-κB |
| 背景说明 |
一种二萜类三环氧化物，具有免疫抑制，抗炎和抗增殖作用。是 NF-κB 活化的抑制剂。 |
| 生物活性 |
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive， anti-inflammatory， antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor.[1-6] |
| In Vitro |
Triptolide 在培养的和原发性慢性淋巴细胞白血病 (CLL) B 细胞中诱导细胞凋亡。用 Triptolide 处理 CD19+ B 细胞，诱导培养的和原代 CLL 细胞凋亡的剂量依赖性增加。Triptolide 对高风险 (n=5) 和低风险 CLL (n=12) B 细胞 (10-50 nM 范围) 具有选择性毒性，同时在很大程度上保留正常 B 细胞 (n=5)。与抑制热休克诱导的 HSP 转录一致，Triptolide 处理可减弱热休克诱导的 HSP 表达[1]。Triptolide 是一种源自中国植物雷公藤的天然产物，据报道在多种癌症中表现出抗肿瘤作用。Triptolide 以剂量依赖性方式抑制 MDM2 表达，即使在 20-100 nM 的低浓度下，在急性淋巴细胞白血病 (ALL) 细胞中也是如此。Triptolide 在所有 8 种具有天然 MDM2 过表达的细胞系中表现出强烈的细胞毒活性，IC50 值范围为 47 到 73 nM。雷公藤甲素对表达极低水平 MDM2 的 EU-4 细胞的细胞毒性作用要小得多，而当 MDM2 稳定转染时，雷公藤甲素能有效杀死这些细胞 (IC50 值：725 nM 对 88 nM)[2]。分化的 PC12 细胞与不同浓度的 Triptolide (0.01、0.1 和1 nM) 在10 μM Aβ25-35 存在下孵育 24 小时，MTT 法检测雷公藤甲素的作用.结果表明，Aβ25-35可降低细胞活力，Triptolide 处理后分化的PC12细胞活力显著增加。结果表明雷公藤甲素可以减轻 Aβ25-35引起的细胞损伤，说明雷公藤甲素具有神经保护作用[3]。 |
| In Vivo |
小鼠接受静脉注射后 Triptolide (TP) 血浆浓度迅速下降。注射 2 小时后，所有三组的 Triptolide 浓度均降至低于定量下限。在对照组和处理组之间进行参数比较，以评估 P-gp 抑制对 Triptolide 暴露和消除的影响。mdr1a-siRNA处理可显著增加雷公藤甲素血浆暴露，Cmax从 413±74 增加到510±94 ng/mL (P[4]。 |
| 细胞实验 |
The viability of differentiated PC12 cells treated with different concentrations of Triptolide. After differentiated PC12 cells are cultured on 96-well plates with RPMI 1640 medium for stabilization， differentiated PC12 cells are incubated with different concentrations of Triptolide (0.01， 0.1， and 1 nM) for 24 hours. The concentrations in this study are chosen. Then cell viability is determined by the MTT assay. Each condition and experiment is repeated three times[3]. |
| 动物实验 |
Mice[4]Male BALB/C mice (weight， 18-22 g) are used. For Triptolide (TP) plasma kinetic study and toxicological evaluation， mice are divided into four groups (n=5 each) to collect blood and tissue samples: (1) normal+saline group; (2) 1.0 mg/kg Triptolide+15 nmol negative control (NC) siRNA-siRNA group; (3) 1.0 mg/kg Triptolide+15 nmol mdr1a-siRNA group; (4) 1.0 mg/kg Triptolide+10 mg/kg Tariquidar group. In order to avoid the complication caused by drug absorption or possible intestinal first-pass effect， Triptolide and the inhibitor are intravenously administrated to mice. The siRNA group is intravenously injected with NC-siRNA or mdr1a-siRNA 2 days before Triptolide dose. For Triptolide+Tariquidar group， the mice are received an intravenous Tariquidar dose 20 min prior to the Triptolide injection. Blood samples are collected at 2， 5， 10， 15， 30， 60 and 120 min after Triptolide dosing. To assess the liver exposure of Triptolide， liver tissue samples are collected from another set of mice at 5， 30， 60 and 120 min after dosing. Three Triptolide groups are design for this experiment， including Triptolide+NC-siRNA group， Triptolide+mdr1a-siRNA group and Triptolide+Tariquidar group. The liver tissue samples are weighed and then homogenized in 10 volume (w:v) of ice-cold saline. The concentrations of Triptolide in plasma and liver tissue are measured by a validated LC-MS/MS method. |
| 数据来源文献 |
[1]. Ganguly S， et al. Targeting HSF1 disrupts HSP90 chaperone function in chronic lymphocytic leukemia. Oncotarget. 2015 Oct 13;6(31):31767-79.
[2]. Huang M， et al. Triptolide inhibits MDM2 and induces apoptosis in acute lymphoblastic leukemia cells through a p53-independent pathway. Mol Cancer Ther. 2013 Feb;12(2):184-94.
[3]. Xu P， et al. Triptolide Inhibited Cytotoxicity of Differentiated PC12 Cells Induced by Amyloid-Beta25-35 via the Autophagy Pathway.
PLoS One. 2015 Nov 10;10(11):e0142719.
[4]. Kong LL， et al. Inhibition of P-glycoprotein Gene Expression and Function Enhances Triptolide-induced Hepatotoxicity in Mice.
Sci Rep. 2015 Jul 2;5:11747.
[5]. Zhang W， et al. Triptolide Combined with Radiotherapy for the Treatment of Nasopharyngeal Carcinoma via NF-κB-Related Mechanism. Int J Mol Sci. 2016 Dec 19;17(12). pii: E2139.
[6]. Cai J， et al. Natural product triptolide induces GSDME-mediated pyroptosis in head and neck cancer through suppressing mitochondrial hexokinase-ΙΙ. J Exp Clin Cancer Res. 2021;40(1):190. Published 2021 Jun 9. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
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