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℃
Dehydroandrographide Succinate Potassium Salt (CAS number: 76958-99-1) is a natural derivative derived from the Chinese medicinal herb Andrographis paniculata, which has attracted much attention due to its significant anti-inflammatory activity. Chuanxinlian, as a widely used traditional Chinese medicine herb for clearing heat and detoxifying, has one of its main active ingredients, Chuanhuning. In recent years, with the deepening development of natural product pharmacology, Chuanhuning has shown unique pharmacological potential in anti-inflammatory, immune regulation, and treatment of related diseases. This article will provide a systematic review of the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity and mechanism of action, pharmacological evaluation and pharmacokinetic characteristics of Chuanhuning, and explore its clinical application prospects, aiming to provide theoretical basis and reference for further research and development of this natural product.
The chemical name of Chuanhuning is dehydroandrographolide succinate potassium salt, with a molecular formula of C26H34K2O10 and a molecular weight of 532.5860. Its structure is based on the andrographolide skeleton, which is modified with succinate to form potassium salt, enhancing its water solubility and bioavailability. The LogP value of Chuanhuning is 2.7913, indicating that it has moderate lipid solubility and is beneficial for cell membrane permeation; The TPSA (topological polar surface area) is 153.5 Å ², indicating high polarity and meeting the requirements for drug molecule target binding. The water solubility is 0.0762, which is not high but has been improved compared to andrographolide, which is beneficial for the development of formulations. Chuanhuning has low blood-brain barrier permeability, reducing the risk of central nervous system side effects. The hERG channel inhibition test was negative, indicating a low risk of cardiac toxicity. The Ames mutagenicity test result is 0, indicating that the toxicity risk of Chuanhuning gene is extremely low and the safety is good.
The molecular structure of Chuanhuning contains multiple hydroxyl and ester bonds, endowing it with excellent chemical reactivity and biocompatibility. Its structural characteristics enable it to form stable binding with various inflammation related target molecules, thereby exerting anti-inflammatory and immune regulatory effects.
The natural precursor of Chuanhuning, Andrographis paniculata, mainly exists in the traditional Chinese medicine Andrographis paniculata. Andrographis paniculata is a plant of the Scrophulariaceae family, widely distributed in tropical and subtropical regions of Asia. Traditionally, Chuanxinlian is used to treat colds, fever, inflammation, and gastrointestinal diseases. Chuanhuning, as a derivative of Chuanxinlian lactone, is usually obtained through chemical modification.
The extraction of Chuanxinlian is usually carried out using ethanol or methanol as solvents, and crude extracts are obtained through reflux extraction or ultrasound assisted extraction methods. Subsequently, through liquid-liquid distribution, column chromatography and other separation and purification techniques, andrographolide was isolated. Chuanhuning improves its water solubility and stability by performing succinic acid esterification reaction on Chuanxinlian lactone, followed by neutralization to generate potassium salt form.
Modern preparation processes emphasize green environmental protection and efficient separation, using supercritical CO2 extraction, membrane separation technology, and high-performance liquid chromatography (HPLC) purification to ensure the purity of Chuanhuning and the stability of its active ingredients, laying the foundation for its drug development.
The main pharmacological activity of Chuanhuning is focused on anti-inflammatory effects, and it also exhibits immunomodulatory, antioxidant, and anti-tumor potential. A large number of in vitro cell experiments and in vivo animal model studies have confirmed its significant anti-inflammatory effect.
Chuanhuning reduces inflammation by inhibiting the production and release of various inflammatory mediators. Its targets include pro-inflammatory cytokines IL-6, TNF - α, inflammatory signal transduction factor STAT3, inflammation related enzymes PTGS1 (COX-1), PTGS2 (COX-2), NOS2 (iNOS), etc. Chuanhuning can significantly reduce the expression and activity of these targets, inhibit the synthesis of inflammatory mediators, and alleviate cytokine storms and tissue damage.
Chuanhuning regulates immune cell function and promotes immune homeostasis. Research has found that it has a regulatory effect on the activation and secretion functions of macrophages and T cells, can balance Th1/Th2 immune responses, and reduce inflammatory damage caused by immune overactivation.
Chuanhuning has the ability to eliminate free radicals, reduce oxidative stress levels, and protect cells from oxidative damage. Its antioxidant mechanism is closely related to regulating the Nrf2 signaling pathway, promoting the expression of antioxidant enzymes.
Some studies have shown that Chuanhuning has a regulatory effect on TRPV1 and TRPA1 channels, which may be involved in pain transmission and neuroinflammatory processes. In addition, Chuanhuning exhibits inhibitory activity on proliferation and induces apoptosis in certain tumor cells, indicating its potential application value in the field of anti-tumor.
The anti-inflammatory mechanism of Chuanhuning involves multiple signaling pathways and molecular targets, mainly including:
Chuanhuning blocks the inflammatory cascade 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 response, is closely associated with overexpression in various chronic inflammatory diseases. Chuanhuning reduces inflammation by inhibiting IL-6 signaling.
STAT3 is an important transcription factor that mediates cell proliferation, differentiation, and inflammatory response. Chuanhuning inhibits the phosphorylation and nuclear translocation of STAT3, blocks its downstream gene expression, and suppresses abnormal activation of inflammation and immune response.
Chuanhuning 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 that regulates the expression of inflammatory genes. Chuanhuning achieves anti-inflammatory effects by blocking the degradation of I κ B α, inhibiting the nuclear translocation of NFKB1, and reducing the transcription of inflammatory genes.
Chuanhuning has a regulatory effect on TRPV1 and TRPA1 channels, reducing the transmission of neuroinflammation and pain signals, and alleviating inflammation related pain.
CASP1 (inflammasome associated caspase 1) is involved in the activation of inflammasomes and the maturation of IL-1 β. Chuanhuning inhibits CASP1 activity and blocks inflammasome mediated inflammatory responses.
In summary, Chuanhuning exerts its broad-spectrum anti-inflammatory and immune regulatory functions through multi-target and multi pathway synergistic effects, providing a solid molecular basis for its clinical application.
The pharmacological parameters of Chuanhuning indicate that it has good potential for drug development. The molecular weight of 532.5860 is within an acceptable range, with a LogP of 2.79, indicating that it has moderate lipid solubility and is beneficial for oral absorption. The TPSA is 153.5, indicating that its polarity is moderate and conducive to binding to the target. Although its water solubility is not high (0.0762), as a potassium salt form, its water solubility is significantly improved compared to andrographolide, making it easier for formulation design.
Chuanhuning has low blood-brain barrier permeability, reducing the risk of central nervous system toxicity. The negative hERG channel inhibition test indicates low risk of cardiac toxicity and high safety. The Ames test result is 0, indicating a very low risk of genetic toxicity.
In terms of pharmacokinetics, existing studies have shown that Chuanhuning is well absorbed after oral administration, with a moderate plasma half-life, mainly metabolized through the liver, and excreted through urine and bile. Further research is needed on the activity of its metabolites. The bioavailability of Chuanhuning is limited by the first pass effect, and its pharmacokinetic performance can be improved in the future through novel drug delivery systems such as nanocarriers and liposomes.
Chuanhuning has broad clinical application prospects due to its significant anti-inflammatory activity and good safety. Its potential indications include:
Inflammatory diseases Such as rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease (COPD), etc., Chuanhuning is expected to alleviate symptoms and prevent disease progression by inhibiting inflammatory mediators and signaling pathways.
infectious diseases Chuanhuning has shown potential in antiviral and antibacterial adjuvant therapy, especially in exerting immunomodulatory effects in virus induced inflammatory responses.
Neuroinflammation and Pain Management By regulating TRPV1 and TRPA1 channels, Chuanhuning may become a candidate drug for neuroinflammation and chronic pain.
neoadjuvant therapy The anti-tumor activity of Chuanhuning provides new ideas for its regulation and adjuvant therapy in the tumor inflammatory microenvironment.
Future research should focus on the clinical trial design of Chuanhuning, clarifying its effective dosage, safety, and treatment window. At the same time, in-depth analysis of its molecular mechanism, optimization of formulation process, and improvement of bioavailability and targeting. Multidisciplinary joint research will promote the transition of Chuanhuning from laboratory to clinical application, benefiting patients.
As a derivative of Chuanxinlian lactone, Chuanhuning has demonstrated excellent pharmacological activity and potential as a drug 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 treatment. The drug efficacy evaluation shows that Chuanhuning has good safety and pharmacokinetic characteristics, and is suitable for further development as a clinical drug. In the future, through systematic pharmacological, toxicological, 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.
