Triptolide
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Triptolide是从中药雷公藤中提取出来的主要生物活性成分。
Triptolide抑制活化T细胞中的IL-2表达,以及NF-κB介导的转录激活[1]。在极低浓度下,Triptolide也可以抑制集落形成与肿瘤细胞增殖。
给予15 nM的Triptolide可以抑制卵巢癌细胞SKOV3和A2780的侵袭和迁移。Triptolide在0 ~ 15 nM的浓度下,呈剂量依赖性地抑制卵巢癌细胞内的MMP7和MMP19表达。Triptolide也可以增强卵巢癌细胞中的E-钙黏蛋白表达,从而影响迁移过程与细胞侵袭[2]。Triptolide在100 nM的最低剂量下,呈剂量依赖性地减少Rpb1,导致SKOV3细胞中的RNAPII显著减少[3]。在类风湿滑膜成纤维细胞(RSF)中,Triptolide呈剂量依赖性地显著降低细胞活力(IC50 = 74.3 nM),同时抑制细胞增殖(IC50 = 20.4 nM)。给予Triptolide(100 nM),持续24小时,可以显著改变滑膜细胞形态[4]。Triptolide在10 ~ 100 ng/ml的浓度下,通过增加DEVD裂解的caspases活性,诱导外周T细胞和T细胞杂交瘤的凋亡性死亡。[5]
在原代人滑膜成纤维细胞、SW1353细胞和人骨关节炎软骨细胞中,125 ~ 150nM的Triptolide抑制细胞因子诱导的MMP-3表达,从而阻止聚集蛋白聚糖酶和MMP驱动的软骨分解[6]。
参考文献:
[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.
- 1. Lei Zhang, Jianyi Gao, et al. "Microvesicles Derived from Human Embryonic Neural Stem Cells Inhibit the Apoptosis of HL-1 Cardiomyocytes by Promoting Autophagy and Regulating AKT and mTOR via Transporting HSP-70." Stem Cells International. Volume 2019, Article ID 6452684, 15 pages.
- 2. 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
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 360.41 |
Cas No. | 38748-32-2 |
Formula | C20H24O6 |
Synonyms | PG490 ;PG 490 ;PG-490 |
Solubility | ≥36 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
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 |
SDF | Download SDF |
Canonical SMILES | C[C@@]12[C@@]34[C@@]5([C@H](O)[C@@]6(C(C)C)O[C@H]6[C@@H]3O4)O[C@H]5C[C@]1(C(COC7=O)=C7CC2)[H] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
质量控制和MSDS
- 批次: