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Product name: Wilforlide A
Synonym name: Abruslactone A; Regelide
Catalogue No.: BP1452
Cas No.: 84104-71-2
Formula: C30H46O3
Mol Weight: 454.695
Botanical Source: Tripterygium wilfordii Hook.f.
Physical Description:
Type of Compound: Triterpenoids
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.
The product could be supplied from milligrams to grams
Inquire for bulk scale.
Description:
Wilforlide A is a quality control standard of Tripterygium Glycosides that be listed in Drug Standard of Ministry of Public Health of the People's Republic of China. Wilforlide A has obvious anti-inflammatory effects.
References:
Fitoterapia. 2010 Dec;81(8):1109-12.
Comparative study on the anti-inflammatory and immune suppressive effect of Wilforlide A.
Tripterygium Glycosides (TG) is effective in the treatment of patients with a variety of inflammatory and autoimmune diseases, especially rheumatoid arthritis (RA) in clinical. Wilforlide A (T(1)) serves as a quality control standard of TG that be listed in Drug Standard of Ministry of Public Health of the People's Republic of China. The pharmacologic actions of T(1) remain to be unidentified.
METHODS AND RESULTS:
In this paper, we studied the anti-inflammatory and immune suppressive effect of T(1), and compared it with Triptolide (TP), which believed to be the major active component of TG. Carrageenan-induced rat pedal swelling, tampon-induced rat granulation, and mice ear inhibition rate of swelling trail results show that high-dose T(1) has obvious anti-inflammatory effect. Colorimetric detection contents of hemolysin, carbon elimination from plasma of mice, mice delayed hypersensitivity immune, and organ index were measured.
CONCLUSIONS:
The results show that T(1) has no significant immune suppressive activity, and there has a significant difference with TP and TG. Therefore, we think the content of TP also should be controlled as a supplement standard in order to ensure safe and effective medication.
HPLC of Wilforlide A
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
46.5300
6.6454
6.6449
.0004
6.6710
13.2445
High
90.6646
5.7795
No
No
No
No
Yes
No
0.0
No
No
No
Yes
Wilforlide A is a type of medicinal herb derived from the medicinal herb Tripterygium wilfordii Hook. f.) As an important anti-inflammatory and immune-regulating herb in traditional Chinese medicine, Thunder Vines has attracted much attention due to its remarkable pharmacological activity. As one of its main active components, Trigmatolide A demonstrates significant anti-inflammatory and immunosuppressive effects, making it a hot topic in pharmacological research of natural products. In recent years, with advances in molecular biology and pharmacological techniques, the mechanism of action and molecular targets of Trigmatolide A have gradually been clarified, providing a theoretical foundation for its clinical application and new drug development.
This paper will systematically review the chemical structure and physicochemical properties of Trigmatolide A, plant origin and extraction methods, pharmacological activity and mechanism, druggability evaluation, and pharmacokinetic characteristics, combined with its potential applications in immunosuppressive diseases, to explore its clinical development prospects and future research directions.
Wilforlide A (CAS No.: 84104-71-2) is a triterpene compound with the molecular formula C30H46O4 and a molecular weight of 454.6950. Its structure includes a typical triterpene skeleton, featuring multiple ring-like structures and functional groups, giving it unique biological activity. The LogP value of Triptella lactone A is 6.6454, indicating strong lipid solubility, and the TPSA (Topological Polarity Surface Area) is 46.53, indicating moderate polarity that facilitates cell membrane penetration. Its water solubility is extremely low (0.0004), suggesting poor solubility in the body and potentially affecting its bioavailability.
Additionally, Trigonolide A can effectively cross the blood-brain barrier (BBB), which opens up potential applications in central nervous system diseases. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames mutagenic test scored 0.0, indicating a low genotoxicity risk and high safety.
Tripterygium wilfordii Hook. f.) is a traditional Chinese medicinal herb widely distributed in China and East Asia. Trigodium is renowned for its remarkable anti-inflammatory, immunomodulatory, and antitumor activities, and has long been used to treat immune-related diseases such as rheumatoid arthritis and systemic lupus erythematosus.
Common methods for extracting Tritullis lactone A include solvent extraction, column chromatography separation, and high-performance liquid chromatography (HPLC) purification. The typical process is as follows:
In recent years, new technologies such as supercritical fluid extraction and microwave-assisted extraction have also been attempted to extract Trigium lactone A, aiming to improve extraction efficiency and purity, reduce solvent usage, and promote the development of green pharmaceutical processes.
Trigonolide A, as an important active component in Trigonolide, exhibits multiple pharmacological activities, with anti-inflammatory and immunosuppressive effects being the most prominent.
Both in vitro and in vivo experiments have shown that Trigonolide A can significantly inhibit the production and release of inflammatory mediators. For example, in macrophage and monocyte models, Trigolide A inhibits the expression of pro-inflammatory cytokines such as tumor necrosis factor α (TNF-α) and interleukin-6 (IL-6), reducing inflammatory responses. Additionally, it exerts anti-inflammatory effects by inhibiting activation of the nuclear factor κB (NF-κB) signaling pathway, reducing the transcription level of inflammatory genes.
Trigmatolide A has a regulatory effect on the immune system, especially showing inhibitory effects in T cell-mediated immune responses. It can inhibit T cell proliferation and activation, reduce the secretion of pro-inflammatory cytokines such as interferon γ (IFN-γ) and interleukin-2 (IL-2), while also promoting the expression of regulatory T cell (Treg) related factors like FOXP3, thereby maintaining immune homeostasis.
Additionally, Trigium lactone A regulates the calcineurin (PPP3CA) and nuclear factor-activated T cell (NFATC1) signaling pathways, helping to inhibit excessive activation of immune cells and alleviate the pathological progression of autoimmune diseases.
Some studies have shown that Trigonolide A also possesses certain antitumor activity, possibly by inducing tumor cell apoptosis and suppressing inflammatory responses in the tumor microenvironment. Additionally, it has certain effects on the central nervous system, possibly related to its high blood-brain barrier permeability, but related research is still in its early stages.
The mechanism of action of Trigmatolide A mainly involves multiple signaling pathways and key molecular targets, reflecting its multi-target and multi-pathway regulation characteristics.
Signal transduction and transcription activator factor 3 (STAT3) is a key regulator of various immune and inflammatory responses. Trigmatolide A can inhibit STAT3 phosphorylation and nuclear translocation, block the expression of its pro-inflammatory genes, and reduce inflammatory responses and immune cell activation.
NF-κB is a core transcription factor regulating immune and inflammatory responses. Trigmatolide A exerts anti-inflammatory and immunosuppressive effects by inhibiting the degradation of IκBα, preventing NF-κB from entering the nucleus, reducing the expression of pro-inflammatory cytokines, and exerting anti-inflammatory and immunosuppressive effects.
Trigolydon lactone A regulates the expression of various cytokines, including:
Trigolydon lactone A promotes FOXP3 expression, enhances the function of regulatory T cells, helps maintain immune balance, and prevents excessive activation of autoimmune responses.
By regulating the calcium-binding protein CALN1 and calcineurin (PPP3CA), Trigium lactone A influences NFATC1 activity, inhibiting T cell activation and cytokine production.
In summary, Trigmatolide A demonstrates excellent immunomodulatory potential by coordinating multiple targets to regulate immune and inflammatory signaling pathways.
The druggability evaluation of Trigmatolide A shows that it has certain advantages and challenges.
The high lipid solubility of Trigonolide A (LogP=6.6454) aids in cell membrane penetration and tissue distribution, especially its ability to cross the blood-brain barrier, expanding its application potential in central nervous system diseases. However, its extremely low water solubility (0.0004) limits its oral absorption and bioavailability, requiring formulation improvements (such as nanocarriers, liposomes, etc.) to enhance its release and absorption efficiency in vivo.
The hERG channel inhibition test was negative, indicating a low cardiotoxicity risk for Triglosia lactone A. A negative Ames test indicates low genotoxicity risk and good safety, providing strong support for clinical development.
Existing studies indicate that Trigonolide A is widely distributed in the body, especially enriched in immune-related tissues. Its metabolic pathway mainly involves hepatic enzyme systems, and the activity and toxicity of these metabolites require further research. It has a moderate half-life, suitable for maintaining therapeutic concentration after multiple doses.
In the future, systematic research on its pharmacokinetic parameters, including absorption, distribution, metabolism, excretion (ADME), and drug interactions, is needed to provide a basis for clinical dose design and safety evaluation.
Trigonolide A, as a natural triterpene immunomodulator, has broad clinical application prospects. Its significant anti-inflammatory and immunosuppressive effects give it potential value in various immune-related diseases, especially in rheumatoid arthritis, systemic lupus erythematosus, and transplant rejection.
Trigonolide A regulates multiple immune signaling pathways, inhibits inflammatory cytokines and immune cell activation, effectively reducing joint inflammation and tissue damage. In the future, combined with modern drug delivery technologies, it is expected to develop into a safe and effective new immunosuppressant.
Its promoting effect on regulatory T cells and enhancing immune tolerance suggest that Trigmatolide A has potential in immunosuppression and rejection prevention during organ transplantation.
With its high blood-brain barrier penetration ability, Trigolide A may play a role in immune-related central nervous system diseases such as multiple sclerosis and neuroinflammation, making it worthy of in-depth study.
Although Trigmatolide A has good pharmacological activity and safety advantages, its poor water solubility and low bioavailability are the main bottlenecks in clinical application. In the future, focus should be placed on developing new formulation technologies, such as liposomal encapsulation and nanoparticle delivery systems, to improve their pharmacokinetic properties and targeting.
In addition, in-depth analysis of the activity and safety of its metabolites and systematic preclinical and clinical studies are key to promoting its translational application.
Trigonolide A, as an important triterpenoid active component in Trigonoli, has become a research hotspot in the field of natural product pharmacology due to its significant anti-inflammatory and immunosuppressive effects. Its multi-target and multi-pathway mechanisms provide new ideas and strategies for the treatment of immune-related diseases. Despite challenges in water solubility and bioavailability, Trigmatolide A still demonstrates good pharmaceutical potential and safety.
In the future, by integrating modern medicinal chemistry, pharmacogenuine, and molecular biology technologies, in-depth research on its pharmacokinetics, pharmacodynamics, and clinical studies will help promote the clinical translation of Trigmatolide A and benefit patients with immune-related diseases. As an important representative of natural product pharmacology, research on Trigolactone A not only enriches natural drug resources but also provides valuable molecular templates and theoretical foundations for new drug development.
Shenshuai
Wenjing
Hedandan
