Product name: Gelsevirine
Synonym name:
Catalogue No.: SBP00064
Cas No.: 38990-03-3
Formula: C₂₁H₂₄N₂O₃
Mol Weight: 352.434
Botanical Source:
Physical Description: Powder
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
The product could be supplied from milligrams to grams. Inquire for bulk scale.
We provide solution to improve the water-solubility of compounds, thereby facilitating the variety of activity tests and clinic uses.

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

Gelsevirine (CAS No.: 38990-03-3) is one of the main alkaloids isolated from the genus Gelsemium elegans. As a traditional Chinese medicinal material, Gouwen has always attracted attention for its remarkable biological activity, especially its potential pharmacological effects in anti-anxiety, analgesia, and anti-tumor properties. As an important active ingredient in this plant, Aconiophyllax has attracted widespread research interest in the field of natural product pharmacology in recent years. Its unique chemical structure and multi-target mechanism make it a novel candidate drug for studying anxiety disorders and related neuropsychiatric disorders. In addition, Hook-nose green alkali exhibits certain anti-proliferative activity against various tumor cells, providing a theoretical basis for its anti-tumor potential.

This review aims to systematically summarize the chemical structure, plant origin, extraction methods, pharmacological activity, and mechanism of action of Hook-sung green alkalis, and, combined with druggability evaluation and pharmacokinetic characteristics, deeply explores its prospects and challenges in clinical application, providing scientific reference for subsequent research and new drug development.

Chemical structure and physicochemical properties

The molecular formula of Hook-Kissed Green Alkali is C20H22N2O3, with a molecular weight of 352.4340. Its structure belongs to the indole alkaloids, featuring a typical polycyclic framework and nitrogen-containing heterocyclic structure. The molecules of Hook-nosed green alkali contain indole rings and multiple oxidative functional groups, structural features that give it strong biological activity. Its LogP value of 2.1823 indicates that the compound has moderate lipid solubility, facilitating lipid membrane penetration, especially the blood-brain barrier (BBB). Its high blood-brain barrier permeability was evaluated, supporting its pharmacological effects in the central nervous system.

The polar surface area (TPSA) of Hook-nosed green alkali is 42.0100, making it a moderately polar compound with a water solubility of 0.4720, indicating limited solubility in the aqueous phase but sufficient to support absorption in the body. Notably, hook-nose green alkali exhibits hERG channel inhibitory activity, suggesting that its electrophysiological safety in cardiac should be carefully evaluated. Additionally, the Ames test result was 1.2, indicating a possible genotoxicity risk that requires further research.

Plant Origins and Extraction Methods

Hook-mouth green alkali mainly comes from Hook-nose (Gelsemium elegans), an evergreen shrub distributed in southern China and Southeast Asia. In traditional medicine, hooked snout is used to treat various diseases, but its toxicity is relatively strong and should be used with caution. As one of the main alkaloids in this plant, Hook-nosed green alkali is relatively abundant.

Common methods for extracting hook-nosed green alkali include solvent extraction, liquid-liquid distribution, and column chromatography separation. Methanol or ethanol is usually used as the initial extraction solvent to obtain a total alkaloid mixture. Subsequently, impurities are removed through acid-base adjustment and liquid-liquid extraction, combined with silica gel column chromatography or high-performance liquid chromatography (HPLC) for further purification, resulting in high-purity hook-kissed green alkali. In recent years, the application of ultrasound-assisted extraction and microwave-assisted extraction technologies has improved extraction efficiency and purity, providing technical support for large-scale production.

Pharmacological activity research

Anti-anxiety effects

The most well-known pharmacological activity of Gosseng-scented green alkali is its remarkable anti-anxiety effect. Multiple in vivo and in vitro experiments have shown that hook-kissed green alkali can effectively reduce anxiety behaviors in animal models, demonstrating good sedative and anti-anxiety activities. It has a wide dosage range and lower side effects compared to traditional anti-anxiety drugs, demonstrating a good safety window for drug efficacy.

Antitumor activity

Hook-nosed green alkali has an inhibitory effect on the proliferation of various tumor cells. The study showed that the IC50 of the human colon cancer cell line SW480 and the gastric cancer cell line MGC80-3 was 1.41 mM and 1.22 mM respectively, indicating that it can significantly inhibit tumor cell growth at high concentrations. This anti-proliferative effect may be related to its induction of apoptosis, disruption of the cell cycle, and inhibition of tumor-related signaling pathways, though the specific mechanism still needs further elucidation.

Analgesic and other neuroprotective effects

Although the analgesic effects of Acolytes chlorine have not been systematically studied, it has potential interactions with various analgesic-related targets (such as TRPV1, CNR1, OPRD1, etc.), suggesting it may have certain analgesic activity. In addition, the regulatory effects of Hook-nosed green alkali on the central nervous system also offer potential applications in neuroprotection and the treatment of psychiatric disorders.

Mechanism of action and molecular targets

The anti-anxiety mechanism of GlyRs is mainly related to its stimulating effect on glycine receptors (GlyRs) in the brain. Glycine receptors, as important inhibitory neurotransmitter receptors in the central nervous system, regulate neural excitability and mood states. Hook-and-snout green alkali activates glycine receptors, enhances inhibitory nerve conduction, and alleviates anxiety symptoms.

Additionally, hook-nose chlorine may act by regulating various neurotransmitter systems, including dopamine receptor (DRD2), opioid receptors (OPRM1, OPRK1, OPRD1), and serotonin transporter protein (SLC6A4). These targets play key roles in emotional regulation, pain transmission, and cognitive functions. The multi-target effects of hook-and-snung green soda help achieve its comprehensive pharmacological effects.

In terms of anti-tumor effects, hook-nose green alkaloid may induce apoptosis and cell cycle arrest by inhibiting tumor cell proliferation-related signaling pathways such as PI3K/Akt and MAPK. Additionally, its regulation of inflammation-related enzymes PTGS1 (COX-1), PTGS2 (COX-2), and TRP channels (TRPV1, TRPA1) may contribute to its anti-inflammatory and analgesic effects.

Druggability evaluation and pharmacokinetics

The physicochemical properties of Abricantosis green alkali show that it has good lipid solubility and blood-brain barrier permeability, making it suitable for the treatment of central nervous system diseases. Its LogP value and TPSA are both within ideal ranges, supporting its oral absorption and brain distribution.

However, hook-and-pepper green alkaloid exhibits hERG channel inhibitory activity, suggesting a possible cardiotoxicity risk, so cardiac safety assessment should be prioritized during drug development. Additionally, Ames test results suggest it may have some genotoxicity, requiring further long-term toxicology and mutagenicity studies.

Currently, pharmacokinetic data on Hook-nose green alkali are relatively limited. Preliminary studies show that its bioavailability is moderate, widely distributed in the body, and especially enriched in brain tissue. Metabolic pathways may involve the hepatic CYP450 enzyme system, and the activity and safety of these metabolites require further research. Excretion mainly occurs via the kidneys and bile pathways.

Prospects and outlooks for clinical applications

As a natural product with significant anti-anxiety activity and potential antitumor effects, Gossenodoline shows promising clinical application prospects. Its highly effective central nervous system penetration and multi-target modulation make it a novel therapeutic candidate for anxiety disorders, depression, and related neuropsychiatric disorders.

Future research should focus on optimizing the safety of Acolytes green alkalis, especially controlling the risks of cardiotoxicity and genotoxicity. At the same time, in-depth analysis of its mechanism of action and pharmacokinetic characteristics will help guide rational dosing design and formulation of administration regimens. By combining modern medicinal chemical methods, structural modification improves its pharmacodynamic and pharmacokinetic properties, enhancing its drug development potential.

In addition, the application of hook-kissed green alkali also holds great potential in tumor treatment. Although its anti-proliferative activity requires further validation in in vivo models, it provides important clues for the development of novel anti-tumor drugs. In the future, emerging technologies such as nanocarriers can be combined to improve bioavailability and targeting, broadening clinical indications.

Conclusion

As an important alkaloid in the Acrophytes, Hook-Nose green alkali shows broad research and application prospects in anti-anxiety, analgesia, and antitumor fields due to its unique chemical structure and multi-target pharmacological activity. Although its safety and pharmacokinetic characteristics still need further improvement, Gouwen green alkali undoubtedly provides valuable resources and ideas for the development of natural product drugs. In the future, through multidisciplinary collaborative research, it is expected that the laboratory translation of Gouwen green alkali will be realized, promoting the development and innovation of natural product pharmacology.