Koumine |
Catalog No.GN10748
One-Click Copy Product Info
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Koumine is a major active alkaloid extracted from the traditional Chinese medicinal herb Gelsemium elegans, and it exhibits a variety of pharmacological effects, including anti-inflammatory and immunomodulatory activities.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1358-76-5
Sample solution is provided at 25 µL, 10mM.
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Koumine is a major active alkaloid extracted from the traditional Chinese medicinal herb Gelsemium elegans, and it exhibits a variety of pharmacological effects, including anti-inflammatory and immunomodulatory activities[1-2]. Koumine can modulate the activity of multiple signaling pathways, such as NF-κB, MAPK, and PI3K/Akt[3]. Studies have shown that Koumine can alleviate neuropathic pain, suppress neuroinflammation, and protect against neuronal damage[4].
In vitro, treatment of human hepatocellular carcinoma cells (Huh-7 and SNU-449) with Koumine (100–800μg/mL) significantly inhibited cell proliferation and promoted apoptosis. Koumine reduced mitochondrial membrane potential, increased intracellular reactive oxygen species (ROS) levels, and suppressed the phosphorylation of ERK, p38, p65, and IκBα. Additionally, Koumine upregulated the expression of pro-apoptotic proteins cleaved-Caspase-3 and Bax, while downregulating the anti-apoptotic protein Bcl-2[5]. In RAW264.7 macrophages, pretreatment with Koumine (100–400μg/mL) significantly inhibited lipopolysaccharide (LPS)-induced inflammatory responses. Koumine reduced the expression of inducible nitric oxide synthase (iNOS) and the production of nitric oxide (NO), and decreased the secretion levels of pro-inflammatory cytokines interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α). Koumine also inhibited the phosphorylation of p65 and IκBα in the NF-κB signaling pathway and reduced NF-κB DNA-binding activity. Furthermore, Koumine significantly suppressed the phosphorylation of extracellular signal-regulated kinase (ERK) and p38 mitogen-activated protein kinase (p38 MAPK)[6].
In vivo, oral administration of Koumine (0.6–15mg/kg/day) to rats with adjuvant-induced arthritis (AIA) and collagen-induced arthritis (CIA) significantly reduced arthritis index scores, mechanical hyperalgesia, and paw swelling. Koumine also inhibited abnormal increases in thymus and liver weights and improved joint space narrowing and bone destruction. Moreover, Koumine significantly decreased the protein and mRNA expression levels of pro-inflammatory cytokines IL-1β and TNF-α in serum and joint tissues, and suppressed the elevation of anti-type II collagen antibodies (anti-CII IgG) in serum [7]. In a Sprague-Dawley (SD) rat model of non-alcoholic fatty liver disease (NAFLD) induced by a high-fat diet, Koumine (0.056, 0.28, and 1.4mg/kg) was administered intraperitoneally once daily for two weeks starting from the 16th week of model establishment. Koumine dose-dependently and significantly reduced serum levels of triglycerides (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), alanine aminotransferase (ALT), and aspartate aminotransferase (AST), while increasing high-density lipoprotein cholesterol (HDL-C) levels. Koumine also decreased the liver index, improved hepatic steatosis, and significantly reduced the production and mRNA expression of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, IL-17A, IFN-γ) in the liver, while increasing the expression of the anti-inflammatory cytokine IL-10. Additionally, Koumine modulated the proportions of CD4⁺ T cell subsets in the liver, inhibited the differentiation of Th1 and Th17 cells, and promoted the generation of Th2 and Treg cells, thereby exerting immunomodulatory effects and significantly alleviating the pathological progression of NAFLD[8].
References:
[1] Shoaib RM, Zhang JY, Mao XF, et al. Gelsemine and koumine, principal active ingredients of Gelsemium, exhibit mechanical antiallodynia via spinal glycine receptor activation-induced allopregnanolone biosynthesis. Biochem Pharmacol. 2019 Mar;161:136-148.
[2] Xiong B, Jin G, Xu Y, et al. Identification of Koumine as a Translocator Protein 18 kDa Positive Allosteric Modulator for the Treatment of Inflammatory and Neuropathic Pain. Front Pharmacol. 2021 Jun 24;12:692917.
[3] Lin SK, Chen ST, Zhan Y, et al. The alleviatory effects of koumine on MSU-induced gouty arthritis via the TLR4/NF-κB/NLRP3 pathway. Basic Clin Pharmacol Toxicol. 2024 Aug;135(2):133-147.
[4] Xiong B, Zhong Z, Chen C, et al. The anxiolytic effect of koumine on a predatory sound stress-induced anxiety model and its associated molecular mechanisms. Phytomedicine. 2022 Aug;103:154225.
[5] Yuan Z, Liang Z, Yi J, et al. Koumine Promotes ROS Production to Suppress Hepatocellular Carcinoma Cell Proliferation Via NF-κB and ERK/p38 MAPK Signaling. Biomolecules. 2019 Oct 2;9(10):559.
[6] Guo J, Ding W, Cai S, et al. Polydatin radiosensitizes lung cancer while preventing radiation injuries by modulating tumor-infiltrating B cells. J Cancer Res Clin Oncol. 2023 Sep;149(12):9529-9542.
[7] Yang J, Cai HD, Zeng YL, et al. Effects of Koumine on Adjuvant- and Collagen-Induced Arthritis in Rats. J Nat Prod. 2016 Oct 28;79(10):2635-2643.
[8] Yue R, Jin G, Wei S, et al. Immunoregulatory Effect of Koumine on Nonalcoholic Fatty Liver Disease Rats. J Immunol Res. 2019 Feb 17;2019:8325102.
| Cell experiment [1]: | |
Cell lines | Human hepatocellular carcinoma (HCC) cells (Huh-7 and SNU-449) |
Preparation Method | Huh-7 and SNU-449 cells were cultured in DMEM or RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) at 37°C in 5% CO₂. Upon reaching the logarithmic growth phase, cells were treated with Koumine at various concentrations (100, 200, 400, and 800μg/mL) for 24 hours. |
Reaction Conditions | 100, 200, 400, and 800μg/mL; 24 hours. |
Applications | Koumine significantly inhibited HCC cell proliferation in a dose-dependent manner. Koumine also promoted apoptosis, and upregulation of pro-apoptotic proteins (cleaved caspase-3 and Bax) with concurrent downregulation of anti-apoptotic protein Bcl-2. Additionally, Koumine treatment led to mitochondrial dysfunction (decreased mitochondrial membrane potential) and elevated intracellular ROS levels. These effects were accompanied by inhibition of ERK/p38 MAPK and NF-κB signaling pathways (reduced phosphorylation of ERK, p38, p65, and IκBα). |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Nonalcoholic fatty liver disease (NAFLD) was induced by feeding rats a high-fat diet (containing 1% cholesterol, 0.1% bile salt, 10% lard, 5% egg yolk powder and whole milk powder) for 16 weeks. After 16 weeks, rats were intraperitoneally injected with Koumine (0.056, 0.28, or 1.4mg/kg) or saline once daily for 2 weeks. At the end of the 18th week. |
Dosage form | 0.056, 0.28, and 1.4mg/kg; i.p. |
Applications | Koumine significantly reduced serum levels of triglycerides (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), alanine aminotransferase (ALT), and aspartate aminotransferase (AST), while increasing high-density lipoprotein cholesterol (HDL-C) levels. Koumine decreased liver index and improved hepatic steatosis and inflammatory infiltration. Koumine also reduced the production and mRNA expression of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, IL-17A, IFN-γ) and increased the anti-inflammatory cytokine IL-10. Furthermore, Koumine modulated T cell subsets by decreasing Th1 and Th17 cells and increasing Th2 and Treg cells in the liver, thereby exerting immunomodulatory and anti-inflammatory effects against NAFLD. |
References: | |
| Cas No. | 1358-76-5 | SDF | |
| Canonical SMILES | CN1CC2(C3CC4C5=NC6=CC=CC=C6C52CC1C3CO4)C=C | ||
| Formula | C20H22N2O | M.Wt | 306.4 |
| Solubility | ≥ 29mg/mL in DMSO with ultrasonic | Storage | 4°C, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2637 mL | 16.3185 mL | 32.6371 mL |
| 5 mM | 652.7 μL | 3.2637 mL | 6.5274 mL |
| 10 mM | 326.4 μL | 1.6319 mL | 3.2637 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)