Delving into the Latest Updates on Tripterygium Glycosides with Synapse

Overview

Basic Info

Drug Type

Herbal medicine

Synonyms

tripterygium glycosides

Target

DUSP1 x HSP70 heat-shock proteins

Action

inhibitors

Mechanism

DUSP1 inhibitors(dual specificity phosphatase 1 inhibitors), HSP70 heat-shock proteins inhibitors(HSP70 heat-shock proteins inhibitors)

Therapeutic Areas

Immune System DiseasesCardiovascular DiseasesCongenital Disorders+ [6]

Active Indication

Behcet SyndromeNephrotic SyndromeRheumatoid Arthritis+ [1]

Inactive Indication

Crohn Disease

Originator Organization-

Active Organization

Beijing Hospital of the Ministry of Health

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Tripterygiumwilfordii, a traditional Chinese herbal medicine, has been used for treating autoimmune diseases, including rheumatoid arthritis and systemic lupus erythematosus. Tripterygium glycoside tablets (TGT), derived from this herb, is widely used in clinical practice in China. However, the therapeutic effects of TGT on Multiple sclerosis (MS), particularly through its active component triptolide (TP), remain insufficiently understood.

AIM OF THE STUDY:

This study aimed to investigate the therapeutic effects of TGT and TP on experimental autoimmune encephalomyelitis (EAE) and elucidate the underlying molecular mechanisms.

MATERIALS AND METHODS:

TGT and TWPT were chemically characterized using liquid chromatography coupled with quadrupole time-of-flight mass spectrometry. The therapeutic effect of TGT, TWPT, and TP was evaluated in the EAE model. Proteomics analysis and Western blot analysis were validated the signaling pathways.

RESULTS:

TGT and TP significantly alleviated EAE symptoms in mice, including reduced weight loss and neurological deficits, whereas TWPT (TGT without triptolide) shows no significant therapeutic effect. Histological analysis revealed that TGT and TP reduced demyelination and inflammatory cell infiltration in the spinal cord. TGT and TP decreased systemic inflammatory cytokines (IL-17A, IFN-γ, TNF-α, and IL-6) and the mRNA expression of the transcription factors T-bet and ROR-γt in the spinal cord. Proteomic analysis indicated that TP significantly upregulated the expression of PACAP and activated the cAMP signaling pathway. Furthermore, TGT and TP modulate PKA, PI3K-AKT, NF-κB, and apoptosis-related signaling pathways, contributing to the reducing inflammation, apoptosis and demyelination in EAE mice.

CONCLUSION:

TGT and TP exert anti-inflammatory and demyelination-improving effects to alleviate both clinical and pathological manifestations of EAE in mice via the PACAP/cAMP signaling axis, suggesting TGT as promising therapeutic strategies for MS.

01 May 2025·BIOMEDICAL CHROMATOGRAPHY

Metabolomics Based Exploration of the Mechanism of Action of Tripterygium Glycosides in Diabetic Kidney Disease

Article

Author: Yu, Jianfeng ; Zhang, Jibo ; Long, Li ; Jin, Jingsong

ABSTRACT:

Tripterygium glycosides (TGs), the primary active components of Tripterygium wilfordii, have demonstrated therapeutic efficacy in treating diabetic kidney disease (DKD). However, the precise mechanisms underlying their action remain elusive, limiting the full realization of their medicinal potential. This study employed serum metabolomics based on liquid chromatography–mass spectrometry (LC‐MS) analysis to elucidate the mechanisms by which TGs combat DKD. We evaluated the protective effects of TGs on DKD following treatment. Serum samples were collected before and after treatment, and their metabolic profiles were analyzed using LC‐MS. Our metabolomics analysis revealed that TGs significantly modulated the hedgehog signaling pathway, a key metabolic pathway implicated in DKD pathogenesis. This study represents the first comprehensive investigation of the metabolic pathways regulated by TGs in the context of DKD using a metabolomics approach. Our findings provide a robust theoretical foundation for the more effective utilization and potential combination therapies involving TGs in the management of DKD. These insights pave the way for further research and development of targeted therapeutic strategies for this challenging condition.

01 Jan 2025·INTERNATIONAL IMMUNOPHARMACOLOGY

Therapeutic effects of tripterygium glycosides on periodontitis: Exploring the role of ursolic acid and the RIPK3/NLRP3 signaling pathway

Article

Author: Ren, Long ; Gao, Ying ; Yang, Lina ; Chen, Li

BACKGROUND:

Periodontitis, a chronic inflammatory disease, poses challenges in treatment due to its complex etiology. Tripterygium glycosides (TGs), renowned for their immunosuppressive and anti-inflammatory capabilities, present a prospective therapeutic option for the management of periodontitis. This study delves into the therapeutic efficacy of TGs in periodontitis and reveals the fundamental mechanisms involved.

MATERIALS AND METHODS:

Animal experiments were conducted to observe the therapeutic effects of TGs. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) technology was employed to identify the optimal components. Proteomic technology was used to identify differentially expressed proteins, followed by Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses. Molecular docking and experimental verification of core components and targets were also performed.

RESULTS:

TGs markedly attenuated periodontal damage and alveolar bone resorption and significantly reduced the expression of inflammatory factors. Ursolic acid (UA) was identified as a crucial active ingredient. Among the signaling pathways, the nucleotide-binding oligomerization domain-like receptor (NLR) pathway was the most prominently enriched pathway. The binding of UA to receptor-interacting protein kinase 3 (RIPK3) was demonstrated to have therapeutic efficacy. In vitro experiments verified that UA exerts anti-inflammatory effects through the RIPK3/NLRP3 signaling pathway.

CONCLUSION:

This study demonstrated that TGs effectively treat periodontitis by mitigating alveolar bone loss and suppressing inflammation. As the primary component of TGs, UA exerts therapeutic effects by inhibiting the expression of RIPK3, which in turn influences the activation of the NLRP3 inflammasome and the subsequent expression of downstream inflammatory factors. The findings of this study offer a theoretical foundation for the clinical application of TGs in the management of periodontitis.

100 Deals associated with Tripterygium Glycosides

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