Product name: Koumidine
Synonym name: (19Z)-16-Epinormacusine B
Catalogue No.: BP4694
Cas No.: 1358-75-4
Formula: C₁₉H₂₂N₂O
Mol Weight: 294.398
Botanical Source:
Type of Compound: Alkaloids

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℃

Introduction/Overview

Koumidine (CAS No.: 1358-75-4) is a natural alkaloid isolated from Tripterygium elegans. Plants of the Acornia genus have always held an important position in traditional Chinese medicine, especially for their anti-inflammatory, analgesic, and immunomodulatory effects. As one of the active components in this genus, Acosusin has recently attracted widespread attention in pharmacology and medicinal chemistry due to its significant analgesic activity and multi-target mechanism. This paper aims to systematically review the chemical structure and physicochemical properties of Gotossinsu Wu, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, pharmacokinetic characteristics, and clinical application prospects, providing a theoretical foundation and research direction for subsequent related research and new drug development.

Chemical structure and physicochemical properties

The molecular formula of Goushangsu Wu is C_18H_24N_2O, with a molecular weight of 294.3980. Its structure belongs to the alkaloid class, featuring a typical nitrogen heterocyclic backbone, containing multiple aromatic rings and hydrophobic side chains. The LogP value was 2.4134, indicating moderate lipid solubility, which is beneficial for cell membrane penetration. The polar surface area (TPSA) is 39.26 Ų, indicating moderate polarity and favorable binding to biomacromolecules. Low water solubility (0.1202 mg/mL) suggests limited solubility in the aqueous phase but sufficient to meet certain bioavailability requirements. Hook-and-su sulfate has a high blood-brain barrier penetration ability, indicating it can act on central nervous system targets. Notably, this compound exhibits hERG channel inhibitory activity, suggesting that its cardiac safety should be carefully evaluated. The Ames test result was 0, indicating that Goushan Su Wu had no significant genotoxicity.

Plant Origins and Extraction Methods

Tripterygium elegans mainly originates from Tripterygium elegans, a plant belonging to the Celastraceae family, widely distributed in southern China and parts of Southeast Asia. In traditional Chinese medicine, hooked kiss is used as an anti-inflammatory, analgesic, and immunomodulatory herb. The extraction of Ng-shan-su Pengium is usually done using organic solvent extraction combined with column chromatography separation technology. Specific methods include:

1. Raw material processing: Collect dried Gouwen roots or whole plants, crush into fine powder.
2. Extraction by reflux: methanol or ethanol is used for reflux extraction to extract alkaloid components from plants.
3. Crude extract concentration: Removes solvent by vacuum concentration to obtain a concentrated crude extract.
4. Separation and purification: Using silica gel column chromatography or high-performance liquid chromatography (HPLC) technology, combined with gradient elution, the separation and purification of Ngossu Fenfen.
5. Identification: Confirm compound structure using mass spectrometry (MS), nuclear magnetic resonance (NMR), and infrared spectroscopy (IR).

In recent years, the application of ultrasound-assisted extraction and supercritical fluid extraction technology has further improved the extraction efficiency and purity of Gotosinosu, providing technical support for its large-scale preparation.

Pharmacological activity research

The pharmacological activity of Gouwensu Wu mainly focuses on analgesic effects. Numerous in vivo and in vivo experiments have shown that Gouwensu Wu can significantly reduce pain behaviors in various pain models, including inflammatory pain, neuropathic pain, and chronic pain. Its analgesic effect is comparable to traditional opioids, but its side effects are relatively minor.

In addition, Gouwensu Wu also exhibits certain anti-inflammatory activity, which can inhibit the release of inflammatory mediators and reduce tissue inflammatory responses. Some studies have also found that it has certain antidepressant and anti-anxiety effects, possibly related to its regulation of multiple central nervous system targets.

Specific pharmacological activities include:

• Analgesic effect: In hot plate tests, spinous process stimulation, and chemical pain models, hook-and-sulin protoxin significantly prolonged latency and reduced pain scores.
• Anti-inflammatory effect: Inhibits cyclooxygenase (COX-1/PTGS1 and COX-2/PTGS2) activity, reduces prostaglandin synthesis, and lowers inflammatory responses.
• Neuroprotection: Improves nervous system dysfunction by regulating dopamine receptor (DRD2) and serotonin transporter (SLC6A4) functions.

Mechanism of action and molecular targets

The analgesic mechanism of Hook Essulin is complex, involving regulation of various ion channels, receptors, and enzymes. Its main targets include:

• TRPV1 (Transient Receptor Potential Vanillate Receptor 1): Hookosin can regulate TRPV1 channel activity, inhibit its overactivation, and reduce pain caused by thermal and chemical stimuli.
• TRPA1 (Transient receptor potential vanillin receptor subtype A1): reduces pain sensitivity induced by inflammatory mediators by inhibiting TRPA1 channels.
• CNR1 (Cannabinoid Receptor 1): Hook-and-cannabinoid phenyl may activate or regulate CNR1, exerting analgesic and anti-inflammatory effects.
• OPRD1, OPRM1, OPRK1 (δ, μ, κ-opioid receptors): Multiple bindings of Hook-Nose Sulfate to the opioid receptor family, regulating the endogenous opioid system and exerting central and peripheral analgesic effects.
• PTGS1/PTGS2 (cyclooxygenase 1/2): Inhibits COX enzyme activity, reduces prostaglandin synthesis, and relieves inflammation-related pain.
• SLC6A4 (serotonin transporter): regulates serotonin reuptake, affecting mood and pain perception.
• DRD2 (dopamine D2 receptor): involved in pain regulation and emotional regulation in the central nervous system.

Through multi-target synergistic effects, Gouwensu Wu not only relieves pain but also regulates mood and inflammatory responses, demonstrating its comprehensive advantages as a potential analgesic.

Druggability evaluation and pharmacokinetics

The druggability evaluation of Gouwensu Wu indicates that it has promising potential for drug development. Its molecular weight (294.4) and LogP value (2.41) met the Lipinski rule, suggesting good oral bioavailability. TPSA (39.26 Ų) is moderate, which facilitates cell membrane penetration and blood-brain barrier crossing, supporting central nervous system function.

Low water solubility (0.12 mg/mL) may limit its dissolution rate, but this can be improved through formulation optimization. Its high blood-brain barrier permeability makes it suitable for treating central pain. hERG channel inhibition suggests potential cardiotoxicity risks and requires focused monitoring and optimization in subsequent drug development.

Ames test negative results showed that Acrox-Sulfo-Fenn had no significant mutagenicity and was relatively safe. Preliminary pharmacokinetic studies show that Gouwen is rapidly absorbed orally, has a moderate plasma half-life, and is widely distributed, especially at high concentrations in brain tissue.

Prospects and outlooks for clinical applications

As a natural product of multi-target analgesia, Gouwensu Wu has broad clinical application prospects. Its remarkable analgesic effects and low risk of side effects make it a promising new type of analgesic, especially suitable for treating chronic pain, neuropathic pain, and inflammatory pain.

Future research should focus on:

• Safety Evaluation: In-depth research on the cardiotoxicity mechanisms of Hook Acid Sulfur Acid Sulfate to optimize structure to reduce the risk of hERG channel inhibition.
• Dosage Form Development: Improve water solubility and bioavailability, and develop oral, injectable, and sustained-release formulations.
• Clinical trials: Conduct systematic clinical pharmacology and efficacy evaluations to verify analgesic effects and safety.
• Mechanism research: further elucidates its multi-target synergistic mechanisms and explores other potential indications such as antidepressant and neuroprotection.

In addition, structural modification and derivative development of Gotoshansu Peng will also provide abundant chemical space for new drug development.

Conclusion

As an important alkaloid in the Gotous-no-Plant plant, Goussulin demonstrates excellent analgesic activity and multi-target mechanism, possessing good druggability and high safety potential. Its application prospects in pain management are broad, and through systematic pharmacological, toxicological, and clinical research, it is expected to develop into a new generation of efficient and safe analgesic drugs. Research on Gouwen Suwu not only enriches the theoretical framework of natural product pharmacology, but also provides valuable examples and insights for the development of new natural product drugs.