Triptolide Cas-no-38748-32-2_News

Description:
Triptolide is a diterpene triepoxide antibiotic originally isolated from extracts of the herb Tripterygium wilfordii Hook F (TWHF). Triptolide may act to induce apoptosis of T lymphocytes by activating caspases, displaying an increase of DEVD-cleavable caspase activity correlated with the apoptosis. 
The proliferation of rheumatoid synovial fibroblasts characteristic of rheumatoid arthritis was similarly suppressed by treatment with Triptolide through an increase in caspase-3 activity. 
Cytokine gene expression in blood lymphocytes and T-cells are also suppressed by Triptolide, blocking the transcriptional activation of purine-box/antigen receptor response element/nuclear factor of activated T-cells (NF-AT) and of NF-kappaB.
Triptolide (38748-32-2) possesses potent immunosuppressive and anti-inflammatory activity. Irreversibly inhibits eukaryotic transcription via covalent binding to XPB, a subunit of the transcription factor TFIIH.
1Blocks transactivation of NFkB.2Exhibits potent antiproliferative activity in 60 cancer cell lines (average IC50= 12 nM) and synergizes with other anticancer agents.3Inhibits the inflammatory response and remarkably decreases production of TNF-a, IL-1b and IL-6 in a rat model of rheumatoid arthritis.

Biological Activity:
Inhibits cytokine-induced gene expression via inhibition of NF- κ B transcriptional activity. Induces apoptosis in tumor cells by blocking TNF- α mediated c-IAP2 and c-IAP1 (members of the inhibitor of apoptosis family) induction. Immunosuppressive with anti-inflammatory and antitumor activity.
Biochem/physiol Actions :
Triptolide is a diterpene triepoxide, the principal active ingredient in extracts from the Chinese herb Tripterygium wilfordii hook (TwHF). It is a potent immunosuppressant and anti-inflammatory.
Triptolide has been shown to inhibit the expression of IL-2 in activated T cells at the level of purine-box/nuclear factor and NF-κB mediated transcription activation.
 It synergizes with cyclosporin A in promoting graft survival in animal models and in suppression of graft versus host disease in allogeneic bone marrow transplants.
 In addition, it induces apoptosis in tumor cells and potentiates tumor necrosis factor (TNFα) induction of apoptosis in part through the suppression of c-IAP2 and c-IAP1 induction.

Application and use:
Triptolide exerts its bioactivity by covalently modifying and inhibiting multiple cellular targets, including the XPB subunit of the transcription factor TFIIH, which suppresses RNA polymerase II–mediated transcription, leading to apoptosis in rapidly proliferating cells. 
It also inhibits NF-κB signaling and pro-inflammatory cytokine production.This dual action underlies its potent immunosuppressive, anti-inflammatory, and anticancer effects. 
Potential applications include treatment of autoimmune and inflammatory disorders, such as rheumatoid arthritis, and various malignancies, including pancreatic, breast, and hematologic cancers. 
Its high potency and narrow therapeutic window necessitate careful dosing and targeted delivery strategies in preclinical and clinical development.

Anti-cancer effects:  In recent years, a large number of in vitro and in vivo studies demonstrated this product has good anti-tumor activity to a variety of cancers such as leukemia, breast cancer, pancreatic cancer and lung cancer. 
Recent studies have found that triptolide not only affects certain proteins and signaling pathways specifically, but also inhibits broad gene transcription, but the mechanism remains to be further clarified. 
Triptolide has proven to be an effective synergistic therapy for inhibition of pancreatic cancer cell growth, with IC50 values of 0.01 µM and 0.02 µM in Capan-1 and Capan-2 adenocarcinoma cells, respectively. Triptolide also has shown antiviral efficacy in HIV-1 and dengue virus via inhibition of Tat protein and COX-2, respectively.
Anti-inflammatory and immunosuppressive effects :
Triptolide is an epoxy diterpene lactone compound that extracted from the roots, leaves, flowers and fruits of Tripterygium wilfordii (Celastraceae).  It is insoluble in water, soluble in methanol, dimethyl sulfoxide, ethanol, ethyl acetate, chloroform ect. 
It has anti-inflammatory and immunosuppressive effects: with the application of 10μg/kg sc Triptolide in continuous 10 days, the croton oil-induced ear edema in mice can be reduced.
                   Product manager: Joy Wu                                                      Email address: Joy@coreychem.com