切换导航

Triptolide

现货
Catalog No.
A3891
IL-2/MMP-3/MMP7/MMP19抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,000.00
现货
5mg
¥ 700.00
现货
10mg
¥ 1,200.00
现货
25mg
¥ 2,400.00
现货
1g
¥ 18,000.00
Ship with 10-15 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Triptolide is the major bioactive constituent extracted from the Chinese herb Tripterygium wilfordii.
Triptolide inhibit the expression of IL-2 in activated T cells and NF-κB mediated transcription activation [1]. Triptolide also can inhibit colony formation and the proliferation of tumor cells at extremely low concentrations.
Triptolide treatment at the concentration of 15 nM inhibited the invasion and migration of ovarian cancer cells SKOV3 and A2780. Triptolide inhibited MMP7 and MMP19 expression with a dose-dependent manner from 0 to 15 nM in ovarian cancer cells. Triptolide also enhanced expression of the E-cadherin in ovarian cancer cell, then, affected the migration and cell invation.[2] Triptolide triggered a CDK7-mediated degradation of RNAPII, including its robust anticancer properties. Triptolide induced Rpb1 decrease with a dose-dependent manner at lowest 100 nM, resulting to a significant RNAPII reduction in SKOV3 cells.[3] Triptolide caused significant decrease of cell viability in a dose-dependent manner with IC50 value of 74.3 nM in RSF (rheumatoid synovial fibroblasts). Triptolide also has inhibition effect on cell proliferation in RSF with IC50= 20.4 nM. Treatment with triptolide (100 nM) for 24 h caused distinctive morphological changes in synovial cells.[4] Triptolide induces apoptotic death of peripheral T cells and T cell hybridomas by increase of DEVD-cleavable caspases activity at 10-100 ng/ml.[5]
Triptolide also inhibited cytokine-induced MMP-3 expression at 125-150nM in primary human synovial fibroblasts, SW1353 cells, and human OA chondro-cytes protecting artilage from aggrecanase- and MMP -driven breakdown.[6]
References:
[1].    Qiu D, Zhao G, Aoki Y, Shi L, Uyei A, Nazarian S, Ng JC, Kao PN: Immunosuppressant PG490 (triptolide) inhibits T-cell interleukin-2 expression at the level of purine-box/nuclear factor of activated T-cells and NF-kappaB transcriptional activation. J Biol Chem 1999, 274(19):13443-13450.
[2].    Zhao H, Yang Z, Wang X, Zhang X, Wang M, Wang Y, Mei Q, Wang Z: Triptolide inhibits ovarian cancer cell invasion by repression of matrix metalloproteinase 7 and 19 and upregulation of E-cadherin. Exp Mol Med 2012, 44(11):633-641.
[3].    Manzo SG, Zhou ZL, Wang YQ, Marinello J, He JX, Li YC, Ding J, Capranico G, Miao ZH: Natural product triptolide mediates cancer cell death by triggering CDK7-dependent degradation of RNA polymerase II. Cancer Res 2012, 72(20):5363-5373.
[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].    Yang Y, Liu Z, Tolosa E, Yang J, Li L: Triptolide induces apoptotic death of T lymphocyte. Immunopharmacology 1998, 40(2):139-149.
[6].    Liacini A, Sylvester J, Zafarullah M: Triptolide suppresses proinflammatory cytokine-induced matrix metalloproteinase and aggrecanase-1 gene expression in chondrocytes. Biochem Biophys Res Commun 2005, 327(1):320-327.

文献引用

1. Fong N, Saldi T, et al. "RNA Pol II Dynamics Modulate Co-transcriptional Chromatin Modification, CTD Phosphorylation, and Transcriptional Direction." Mol Cell. 2017 May 18;66(4):546-557.e3. PMID:28506463

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt360.41
Cas No.38748-32-2
FormulaC20H24O6
SynonymsPG490 ;PG 490 ;PG-490
Solubility≥36 mg/mL in DMSO, <2.56 mg/mL in EtOH, <2.46 mg/mL in H2O
Chemical Name(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
SDFDownload SDF
Canonical SMILESCC(C)C12C(O1)C3C4(O3)C5(CCC6=C(C5CC7C4(C2O)O7)COC6=O)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

人卵巢癌细胞系SKOV3和A2780

溶解方法

该化合物在DMSO中的溶解度大于18 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

15 nM, 24-72 h

应用

在SKOV3和A2780细胞中,triptolide(50nM,72h)显著抑制卵巢癌细胞增殖。triptolide(15 nM)在伤后48 h显著抑制细胞迁移。triptolide(15 nM)显著阻断了SKOV3和A2780细胞的侵袭能力。

动物实验[1]:

动物模型

异种移植人卵巢癌细胞系SKOV3的小鼠

给药剂量

口服,0.1、0.3或1 mg/kg/day,每天

应用

在人卵巢癌细胞系SKOV3移植的小鼠中,Triptolide (1 mg/kg)显著减少转移瘤的数量~80%。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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.

质量控制

化学结构

Triptolide

相关生物数据

Triptolide