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Product name: Dehydroandrographolide Succinate Potasium Salt
Synonym name:
Catalogue No.: BP4094
Cas No.: 76958-99-1
Formula: C28H35KO10
Mol Weight: 570.676
Botanical Source: Andrographis Herba
Physical Description: 穿心莲
Type of Compound: Diterpenoids
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.
For Reference Standard and R&D, Not for Human Use Directly.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
153.5000
2.7913
.3512
.0762
2.2524
5.4447
Low
89.3184
5.3492
Yes
Yes
No
No
Yes
No
0.0
No
Yes
Yes
Yes
Dehydroandrographolide Succinate Potassium Salt (CAS No.: 76958-99-1) is a natural derivative derived from the traditional Chinese medicinal herb Andrographis paniculata, attracting attention for its remarkable anti-inflammatory activity. Andrographis paniculata is widely used in traditional Chinese medicine as a heat-clearing and detoxifying herb, with one of its main active ingredients being Chuanhuning. In recent years, with the deepening development of natural product pharmacology, Chuanhuning has demonstrated unique pharmacological potential in anti-inflammation, immunomodulatory, and related disease treatment. This paper systematically reviews the chemical structure and physicochemical properties of transunin, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation and pharmacokinetic characteristics, and explores its clinical application prospects, aiming to provide theoretical basis and reference for further research and development of this natural product.
The chemical name of transhunine is potassium succinate of dehydroandrographolide, with a molecular formula of C26H34K2O10 and a molecular weight of 532.5860. Its structure is based on the andrographolide framework, and potassium salts are formed through succinate esterification, enhancing its water solubility and bioavailability. Transunin's LogP value was 2.7913, indicating moderate lipid solubility that facilitates cell membrane permeation; TPSA (topological pole surface area) was 153.5 Ų, indicating high polarity that meets the requirements for drug molecule binding to targets. Water solubility is 0.0762, which is not high but improves compared to Andrographolide, which is beneficial for formulation development. Transhunin has low blood-brain barrier permeability, reducing the risk of central nervous system side effects. The hERG channel inhibition test was negative, indicating a lower risk of cardiotoxicity. Ames-induced mutagenic test results were zero, indicating that transhunine genotoxicity risk is extremely low and safety is good.
Transhunine's molecular structure contains multiple hydroxyl and ester bonds, giving it excellent chemical reactivity and biocompatibility. Its structural characteristics enable it to stably bind to various inflammation-related target molecules, thereby exerting anti-inflammatory and immunomodulatory effects.
The natural precursor Andrographis paniculata lactone of Paniculin is mainly found in the medicinal herb Andrographis paniculata. Andrographis paniculata belongs to the Scrophulariaceae family and is widely distributed in tropical and subtropical Asia. Traditionally, Andrographis paniculata has been used to treat colds, fevers, inflammation, and gastrointestinal diseases. Transhunine, as a derivative of Andrographolide, is usually obtained through chemical modification.
Andrographis paniculata is usually extracted using ethanol or methanol as solvents, and crude extracts are obtained by reflux extraction or ultrasound-assisted extraction methods. Then, through liquid-liquid separation and column chromatography and other separation and purification techniques, Andrographolide was isolated. Transanesis improves water solubility and stability by succinate esterification of Andrographolide through succinate esterification, which is then neutralized to form potassium salts.
Modern preparation processes emphasize green environmental protection and efficient separation, employing supercritical CO2 extraction, membrane separation technology, and high-performance liquid chromatography (HPLC) purification to ensure transunin's purity and stability of active ingredients, laying the foundation for its drug development.
The main pharmacological activity of transunin is focused on anti-inflammatory effects, and it also exhibits immunomodulatory, antioxidant, and antitumor potential. Numerous in vitro cell experiments and in vivo animal model studies have confirmed its significant anti-inflammatory effects.
Transhuning reduces inflammatory responses by inhibiting the production and release of various inflammatory mediators. Its targets include pro-inflammatory cytokines IL-6 and TNF-α, inflammatory signaling transduction factor STAT3, and inflammation-related enzymes PTGS1 (COX-1), PTGS2 (COX-2), NOS2 (iNOS), and others. Transhunin can significantly reduce the expression and activity of these targets, inhibit the synthesis of inflammatory mediators, and alleviate cytokine storms and tissue damage.
Transane regulates immune cell function and promotes immune homeostasis. Research has found that it regulates the activation and secretion of macrophages and T cells, balancing Th1/Th2 immune responses and reducing inflammatory damage caused by immune overactivation.
Transhunin has the ability to eliminate free radicals and reduce oxidative stress levels, protecting cells from oxidative damage. Its antioxidant mechanism is closely related to the regulation of the Nrf2 signaling pathway, promoting the expression of antioxidant enzymes.
Some studies have shown that transunin modulates TRPV1 and TRPA1 channels, possibly involved in pain conduction and neuroinflammatory processes. Additionally, transunin exhibits activity in inhibiting proliferation and inducing apoptosis in certain tumor cells, suggesting its potential application value in the anti-tumor field.
The anti-inflammatory mechanism of transunin involves multiple signaling pathways and molecular targets, mainly including:
Transhanin blocks inflammatory cascades by downregulating the mRNA and protein expression of pro-inflammatory cytokines such as IL-6 and TNF-α. IL-6, as a key mediator of inflammatory responses, is closely associated with its overexpression and various chronic inflammatory diseases. Transhuning reduces inflammation by inhibiting IL-6 signaling.
STAT3 is an important transcription factor that mediates cell proliferation, differentiation, and inflammatory responses. Transunin inhibits STAT3 phosphorylation and nuclear translocation, blocking downstream gene expression and suppressing abnormal activation of inflammation and immune responses.
Transhunin inhibits the expression and activity of key inflammatory enzymes such as PTGS1 (COX-1), PTGS2 (COX-2), and NOS2 (iNOS), reduces the synthesis of prostaglandins and nitric oxide, and alleviates inflammatory symptoms.
NFKB1 is a core transcription factor regulating the expression of inflammatory genes. Transunin achieves anti-inflammatory effects by blocking IκBα degradation, inhibiting NFKB1 nuclear translocation, and reducing the transcription of inflammatory genes.
Transhunin modulates TRPV1 and TRPA1 channels, reduces neuroinflammation and pain signal transmission, and alleviates inflammation-related pain.
CASP1 (inflammasome-associated caspase 1) is involved in the activation of inflammasome and the maturation of IL-1β. Transhunin inhibits CASP1 activity and blocks inflammatory responses mediated by inflammasomes.
In summary, Chuanhuning leverages its broad-spectrum anti-inflammatory and immunomodulatory functions through multi-target and multi-pathway synergistic effects, providing a solid molecular foundation for its clinical application.
The druggability parameters of transuning indicate its promising potential for drug development. A molecular weight of 532.5860 is within an acceptable range, with a LogP of 2.79, indicating moderate lipid solubility and favorable oral absorption. TPSA was 153.5, indicating moderate polarity, which is favorable for target binding. Although its water solubility is not high (0.0762), as a potassium salt, its water solubility is significantly better than Andrographolide, making it easier for formulation design.
Transhunin has low blood-brain barrier permeability, reducing the risk of central nervous system toxicity. A negative hERG channel inhibition test indicates low cardiotoxicity risk and relatively high safety. The Ames test result was 0, indicating an extremely low genotoxicity risk.
Pharmacokinetics, existing studies show that oral administration of Transhuning is well absorbed, plasma half-life is moderate, mainly metabolized by the liver, and excretion routes include urine and bile. The activity of its metabolites still requires further research. The bioavailability of transanesis is limited by the first-pass effect; in the future, its pharmacokinetic performance can be improved through novel delivery systems such as nanocarriers and liposomes.
With its remarkable anti-inflammatory activity and good safety profile, Chuanhuning has broad clinical application prospects. Its potential indications include:
Inflammatory diseases: such as rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease (COPD), and Chuanhuning, by inhibiting inflammatory mediators and signaling pathways, is expected to relieve symptoms and halt disease progression.
Infectious diseases: Transhanin shows potential in antiviral and antibacterial adjuvant therapies, especially in immunomodulatory effects in virus-induced inflammatory responses.
Neuroinflammation and pain management: By modulating TRPV1 and TRPA1 channels, transenin may become a candidate drug for neuroinflammation and chronic pain.
Tumor adjuvant therapy: The antitumor activity of transhuning offers new ideas for regulating the tumor inflammatory microenvironment and adjuvant therapy.
Future research should focus on clinical trial design for Chuanhuning, clarifying its effective dosage, safety, and therapeutic window. At the same time, it delves into its molecular mechanisms, optimizes formulation processes, and enhances bioavailability and targeting. Multidisciplinary collaborative research will push Chuanhuning from the laboratory to clinical application, benefiting patients.
As a derivative of Andrographolide, transhuning demonstrates excellent pharmacological activity and drug potential due to its unique chemical structure and multi-target anti-inflammatory mechanism. Its multiple roles in regulating inflammatory mediators, signaling pathways, and ion channels provide new strategies for anti-inflammatory and related disease treatments. Druggability evaluation shows that transunin has good safety and pharmacokinetic characteristics, making it suitable for further clinical development. In the future, through systematic pharmacology, toxicology, and clinical research, Chuanhuning is expected to become an important member in the field of natural product anti-inflammatory drugs, promoting the development and innovation of natural product pharmacology.
Shenshuai
Wenjing
Hedandan
