Triptolide
(Synonyms: 雷公藤甲素; PG490) 目录号 : GC14402
雷公藤甲素(Triptolide)是从雷公藤根中提取的二萜类三环氧化物,是 NF-κB 活化的抑制剂。NF-κB是转录因子蛋白复合物家族。
Cas No.:38748-32-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
SKOV3 and A2780 cells |
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Preparation Method |
SKOV3 and A2780 cells were plated in 96-well plates (5 × 103/well). 24h later, triptolide was added to a final concentration of 0, 1.5, 5, 15, 50, or 150 nM for 72 h. |
|
Reaction Conditions |
0, 1.5, 5, 15, 50, or 150 nM; 72 h |
|
Applications |
Triptolide (50nM, 72 h) noticeably inhibited ovarian cancer cell proliferation. Triptolide (15nM) significantly inhibited cell migration 48h after wounding. Triptolide (15nM) markedly blocked the invasive capacity of SKOV3 and A2780 cells. |
| Animal experiment [2]: | |
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Animal models |
orthotopic mouse model |
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Preparation Method |
Mice were then randomized into two treatment groups: (a) control and (b) triptolide-treated mice. Mice were given daily i.p. injections of triptolide (0.2 mg/kg) or vehicle (DMSO) for 60 days. |
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Dosage form |
0.2 mg/kg/d; 60 days; i.p. |
|
Applications |
After a daily injection of triptolide (0.2 mg/kg) for 60 days, the tumor volume was significantly reduced. triptolide also significantly reduced the incidence of local-regional tumor spread. |
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References: [1] Zhao H, Yang Z, Wang X, et al. Triptolide inhibits ovarian cancer cell invasion by repression of matrix metalloproteinase 7 and 19 and upregulation of E-cadherin[J]. Experimental & molecular medicine, 2012, 44(11): 633-641. | |
Triptolide is a diterpene triepoxide isolated for the first time from the medicinal plant Tripterygium wilfordii, exhibiting immunosuppressive, anti-inflammatory, anti-proliferative, and antitumor effects. It acts as an inhibitor of NF-κB activation, where NF-κB is a family of transcription factor protein complexes[1]. Triptolide possesses broad-spectrum anticancer activity, inhibiting the development of colon cancer, breast cancer, renal cell carcinoma, and cervical cancer[2].
In vitro, triptolide (50 nM, 72 h) significantly inhibits the proliferation of ovarian cancer cells SKOV3 and A2780. Triptolide (15 nM, 48h) significantly inhibits cell migration and blocks the invasive capability of cells[2]. Triptolide (50-200 nmol/L) incubated with PANC-1 and MiaPaCa-2 cells significantly reduces cell viability without affecting the viability of normal pancreatic ductal cells[3]. The IC50 value of triptolide on RSF cell viability is 74.3 nM, and its IC50 value on RSF cell proliferation is 20.4 nM[4]. Triptolide (0-150 nM) significantly inhibits the viability of HK1, FaDu, and C666-1 cells in a dose- and time-dependent manner[5].
In vivo, treatment with triptolide (1 mg/kg/d, p.o.) for three weeks in nude mice reduced the number of metastatic nodules by approximately 80%[2]. Triptolide (0.2 mg/kg/d) administered to mice with transplanted pancreatic tumors for 60 days reduced pancreatic cancer growth and significantly decreased local tumor spread[3].
References:
[1] 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).
[2] Zhao H, Yang Z, Wang X, et al. Triptolide inhibits ovarian cancer cell invasion by repression of matrix metalloproteinase 7 and 19 and upregulation of E-cadherin[J]. Experimental & molecular medicine, 2012, 44(11): 633-641.
[3] Phillips P A , Dudeja V , Mccarroll J A ,et al.Triptolide Induces Pancreatic Cancer Cell Death via Inhibition of Heat Shock Protein 70[J].Cancer Research, 2007, 67(19):9407.
[4] Kusunoki N, Yamazaki R, Kitasato H, Beppu M, Aoki H, Kawai S: Triptolide, an active compound identified in a traditional Chinese herb, induces apoptosis of rheumatoid synovial fibroblasts. BMC Pharmacol 2004, 4:2.
[5] 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.
雷公藤甲素(Triptolide)是一种二萜三环氧化物,首次从药用植物雷公藤 (Tripterygium wilfordii) 中分离出来,具有免疫抑制,抗炎,抗增殖和抗肿瘤作用。雷公藤甲素是 NF-κB 活化的抑制剂,NF-κB是转录因子蛋白复合物家族[1]。雷公藤甲素具有广谱抗癌活性,它可以抑制结肠癌、乳腺癌、肾细胞癌和宫颈癌的发生过程[2]。
在体外,雷公藤甲素(50 nM,72 h)显著抑制卵巢癌细胞SKOV 3和A2780的增殖。雷公藤甲素(15 nM,48h)显著抑制细胞迁移,还可阻断细胞的侵袭能力[2]。雷公藤甲素(50-200 nmol/L)与PANC-1 和 MiaPaCa-2 细胞一起孵育,显着降低细胞活力,但对正常胰腺导管细胞活力没有影响[3]。雷公藤甲素对RSF细胞活力的IC50值为74.3 nM,雷公藤甲素对RSF细胞增殖的IC50值为20.4nM[4]。雷公藤甲素(0-150 nM)以剂量和时间依赖性方式显著抑制HK 1、FaDu、C666-1细胞的活力[5]。
在体内,雷公藤甲素(1 mg/kg/d,p.o.)处理三周的裸鼠中,转移结节的数量减少了约 80%[2]。雷公藤甲素(0.2 mg/kg/d)对移植胰腺肿瘤的小鼠治疗60天可减少胰腺癌的生长,并显着减少局部肿瘤扩散[3]。
| Cas No. | 38748-32-2 | SDF | |
| 别名 | 雷公藤甲素; PG490 | ||
| 化学名 | (6aS,7aS,8R,8aR,9aS,9bS,10aS,10bS)-8-hydroxy-8a-isopropyl-10b-methyl-1,5,5b,6,6a,8,8a,9a,9b,10b-decahydrotris(oxireno)[2',3':4b,5;2'',3'':6,7;2''',3''':8a,9]phenanthro[1,2-c]furan-3(2H)-one | ||
| Canonical SMILES | CC(C)C12C(O1)C3C4(O3)C5(CCC6=C(C5CC7C4(C2O)O7)COC6=O)C | ||
| 分子式 | C20H24O6 | 分子量 | 360.41 |
| 溶解度 | ≥ 36 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7746 mL | 13.8731 mL | 27.7462 mL |
| 5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7746 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。