Triptolide

Description

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.1??Blocks transactivation of NFkB.2?Exhibits potent antiproliferative activity in 60 cancer cell lines (average IC50?= 12 nM) and synergizes with other anticancer agents.3?Inhibits the inflammatory response and remarkably decreases production of TNF-a, IL-1b and IL-6 in a rat model of rheumatoid arthritis.4

Chemical properties

White Crystalline Solid

The Uses of Triptolide

Triptolide is a diterpenoid triepoxide with immunosuppressant and antitumor properties.

The Uses of Triptolide

Labelled Triptolite (T815600), diterpenoid triepoxide with immunosuppressant and antitumor properties.

What are the applications of Application

Triptolide is an antiinflammatory immunosuppressive diterpene triepoxide, with antiproliferative and antifertility effects.

Definition

ChEBI: Triptolide is an organic heteroheptacyclic compound, an epoxide, a gamma-lactam and a diterpenoid. It has a role as an antispermatogenic agent and a plant metabolite.

General Description

This substance is a primary reference substance with assigned absolute purity (considering chromatographic purity, water, residual solvents, inorganic impurities). The exact value can be found on the certificate. Produced by PhytoLab GmbH & Co. KG

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.

storage

Store at -20°C

References

1) He?et al. (2015),?Covalent Modification of a Cysteine Residue in the XPB Subunit of the General Transcription Factor TFIIH Through Single Epoxide Cleavage of the Transcription Inhibitor Triptolide; Angew. Chem. Int. Ed. Eng.?54?1859 2) Lee?et al. (1999),?PG490 (Triptolide) Cooperates with Tumor Necrosis factor-α to Induce Apoptosis in Tumor Cells; J. Biol. Chem,?274?13451 3) Qiao?et al. (2016),?Synergistic antitumor activity of gemcitabine combined with triptolide in pancreatic cancer cells; Oncol. Lett.,?11?3527 4) Fan?et al.?(2016),?Triptolide Modulates TREM-1 Signal Pathway to Inhibit the Inflammatory Response in Rheumatoid Arthritis; Int. J. Mol. Sci.?17?498