Tripterygium Wilfordii
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Tripterygium Wilfordii

Tripterygium wilfordii, commonly known as Lei Gong Teng or Thunder God Vine, is a perennial vine celebrated in traditional Chinese medicine for its remarkable therapeutic properties. Historically, it has been utilized to alleviate ailments such as fever, chills, edema, and carbuncles. In recent years, this botanical wonder has garnered significant interest from the scientific community, prompting rigorous investigation into its potential benefits.

The plant is particularly distinguished by its intricate and diverse array of chemical constituents. To date, over 400 natural metabolites have been identified within its composition, including notable categories such as alkaloids, triterpenoids, diterpenoids, and sesquiterpenes. This complexity underpins its myriad pharmacological activities and highlights its potential as a source of novel therapeutic agents.

Typical Active Ingredients

Triptolide

Triptolide, a diterpenoid triepoxide, stands as one of the chief bioactive components of Tripterygium wilfordii. Its pharmacological benefits and potential clinical toxicity have been subjects of extensive research. Triptolide exhibits immunosuppressive, anti-inflammatory, and anti-cancer properties. In tumor cells, it induces apoptosis by inhibiting NF-κB activation, thereby sensitizing the cells to TNF-α-induced programmed cell death. Additionally, triptolide suppresses TGF-β1-induced proliferation and migration in rat airway smooth muscle cells through the inhibition of Smad signaling and NF-κB pathways, respectively.

Celastrol

Molecular structure of celastrol

Celastrol, also known as tripterine, is a chemical compound extracted from the root of Tripterygium wilfordii. This compound is classified as a pentacyclic nortriterpen quinone and belongs to the quinone methide family. Celastrol boasts a wide array of pharmacological properties. Notably, it serves as a potent proteasome inhibitor, targeting the chymotrypsin-like activity of the purified 20S proteasome with an IC50 value of 2.5 μM. Its pharmacological effects include anti-proliferative, anti-inflammatory, anti-tumor, anti-angiogenesis, and antioxidant activities. These multifaceted properties make celastrol a compound of significant interest in medical research and potential therapeutic applications.

Wilfortrine

Wilfortrine is a bioactive sesquiterpene alkaloid known for its immunosuppressive properties. In addition to its immunosuppressive effects, wilfortrine demonstrates several pharmacological activities. Remarkably, it inhibits the growth of leukemia cells in mice and exhibits anti-HIV activity. In studies involving liver cancer cells, particularly the HepG2 cell line, wilfortrine has been shown to induce apoptosis. This pro-apoptotic effect is achieved without altering the cell cycle and is primarily mediated through the upregulation of the pro-apoptotic protein Bax and the downregulation of the anti-apoptotic protein Bcl-2.

Wilforlide A

Wilforlide A is a triterpene isolated from Tripterygium wilfordii and serves as a quality control standard for tripterygium glycosides, a class of drugs derived from the plant. Notably, Wilforlide A exhibits potent anti-inflammatory and immunosuppressive activities. It has been traditionally used as a botanical drug for treating autoimmune diseases such as rheumatoid arthritis (RA), systemic lupus erythematosus (SLE), and psoriasis. Regarding its mechanism of action, Wilforlide A has been shown to inhibit the secretion of pro-inflammatory cytokines, including MCP1, GM-CSF, and M-CSF, as well as suppress the M1 biomarker inducible nitric oxide synthase in synovial cells.

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