| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Koumine does not have a single defined pharmacological target. As an indole alkaloid， it likely interacts with multiple cellular targets to exert its diverse biological activities. It modulates inflammatory pathways, reduces cytokine production, and suppresses microglial M1 polarization. The compound exhibits anti-tumor activity by inducing apoptosis in cancer cells. Its anxiolytic, antistress, and analgesic activities suggest interactions with neurotransmitter systems, possibly GABAergic, serotonergic, or opioid systems. However, the specific molecular targets have not been fully characterized.
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| ln Vitro |
The growth of MCF-7 cells was decreased by kumine (0.5, 1, and 2 mg/mL) in a dose- and time-dependent manner, with an IC50 of 124 µg/mL after 72 hours. Cell cycle arrest in the G2/M phase is brought on by kaumine's induction of apoptosis [1]. In MCF-7 cells, koumine (0.5, 1 and 2 mg/mL) dose-dependently increases the Bax/Bcl-2 ratio and caspase-3 expression [1]. In BV2 cells, LPS-induced microglial M1 polarizing factor protein and mRNA levels are decreased by kumine (25, 50, 100, and 200 μM) [3].
Koumine shows potent anti-tumor, anxiolytic, antistress, antipsoriatic, and analgesic activities. It protects against the development of arthritis in rheumatoid arthritis animal models. Koumine can induce apoptosis of LoVo cells in a time-dependent manner. It inhibits the proliferation of MCF-7 breast cancer cells with an IC50 of 124 µg/ml. The compound modulates inflammatory pathways, reduces cytokine production, and suppresses microglial M1 polarization. Its diverse biological activities make it a versatile research tool in inflammation, pain, and disease-mechanism studies. |
| ln Vivo |
Koumine has a lower level of toxicity; in Wistar rats, its LD50 is 300.0 mg/kg. Rats with adjuvant-induced arthritis (AIA) and collagen-induced arthritis (CIA) show antirheumatic characteristics when given kumine (0.6, 3 or 15 mg/kg/per, po) [2]. At 3 and 15 mg/kg, kumine suppresses the rise in IL-1β blood levels and the cytokine induction in joint tissue and serum TNF-α levels [2]. Koumine (0.28, 7 mg/kg, subcutaneous injection) considerably lessens post-nerve damage neuropathic pain. Iba-1 protein level rise is inhibited by kumine [3].
Koumine protects against the development of arthritis in rheumatoid arthritis animal models. It shows potent anti-tumor, anxiolytic, antistress, antipsoriatic, and analgesic activities. The compound's ability to modulate inflammatory pathways and suppress microglial M1 polarization suggests potential therapeutic applications in inflammatory and neurodegenerative diseases. Its analgesic activity suggests potential for pain management. However, specific in vivo studies beyond arthritis models have not been detailed in the available literature. |
| Enzyme Assay |
No specific non-cell assay protocol is available for Koumine. As a natural product with multiple activities, it could be evaluated in various cell-free assays depending on the specific activity being studied. For anti-tumor activity, enzyme inhibition assays or receptor binding assays could be employed. For anti-inflammatory activity, assays measuring cytokine production or enzyme activity could be used. However, specific protocols have not been detailed in the available literature.
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| Cell Assay |
No specific cell-based assay protocol is available for Koumine. For anti-tumor studies, standard cell-based assays involve treatment of cancer cell lines (e.g., LoVo, MCF-7) with Koumine for 24-72 hours. Cell viability is measured using MTT or CellTiter-Glo assays to determine IC50 values. Apoptosis is assessed by Annexin V/PI staining, caspase activity assays, or DNA fragmentation. For anti-inflammatory studies, microglial cells or macrophages are treated with Koumine, and cytokine production (TNF-α, IL-6, IL-1β) and M1/M2 polarization markers are measured.
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| Animal Protocol |
No specific animal protocol is available for Koumine. For arthritis studies, standard in vivo models include collagen-induced arthritis or adjuvant-induced arthritis in mice or rats. Koumine is administered (route and dose to be determined) for 2-4 weeks. Arthritis severity, joint inflammation, and cytokine levels are assessed. For anti-tumor studies, xenograft models using cancer cell lines could be employed. For analgesic studies, pain models such as formalin test or hot plate test could be used.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for Koumine. The compound has a molecular weight of 306.4 and formula C20H22N2O. The SMILES notation is CN1C[C@]2([C@@H]3C[C@H]4C5=NC6=CC=CC=C6[C@@]52C[C@H]1[C@H]3CO4)C=C. As a small molecule with moderate lipophilicity, it would be expected to have reasonable oral bioavailability and blood-brain barrier penetration. Comprehensive pharmacokinetic studies would be required for therapeutic development.
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| Toxicity/Toxicokinetics |
No detailed toxicology data is publicly available for Koumine. As a natural product， it would require comprehensive toxicological evaluation for therapeutic development. The compound's diverse biological activities suggest potential for both beneficial and adverse effects. The compound is for research use only and not for therapeutic applications.
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| References |
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| Additional Infomation |
Koumine has the molecular formula C20H22N2O and molecular weight 306.4. The chemical name is (3R,7Alpha,20Alpha)-1,19-Tetradehydro-3,17-Epoxy-.... It is a naturally occurring indole alkaloid isolated from Gelsemium elegans. The compound shows potent anti-tumor, anxiolytic, antistress, antipsoriatic, and analgesic activities. It protects against arthritis development in animal models and induces apoptosis of LoVo cells. The compound modulates inflammatory pathways and suppresses microglial M1 polarization. No clinical trial status has been identified.
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| Molecular Formula |
C20H22N2O
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| Molecular Weight |
306.4015
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| Exact Mass |
306.173
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| CAS # |
1358-76-5
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| PubChem CID |
44583834
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
436.5±45.0 °C at 760 mmHg
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| Melting Point |
168℃
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| Flash Point |
217.8±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.763
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| LogP |
2.18
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
615
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CN1C[C@]2([C@@H]3C[C@H]4C5=NC6=CC=CC=C6[C@@]52C[C@H]1[C@H]3CO4)C=C
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| InChi Key |
VTLYEMHGPMGUOT-XMHJOAAQSA-N
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| InChi Code |
InChI=1S/C20H22N2O/c1-3-19-11-22(2)16-9-20(19)13-6-4-5-7-15(13)21-18(20)17-8-14(19)12(16)10-23-17/h3-7,12,14,16-17H,1,8-11H2,2H3/t12-,14+,16-,17-,19-,20-/m0/s1
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| Chemical Name |
(1S,10S,12S,15S,16R,17S)-15-ethenyl-13-methyl-19-oxa-3,13-diazahexacyclo[14.3.1.02,10.04,9.010,15.012,17]icosa-2,4,6,8-tetraene
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~108.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2637 mL | 16.3185 mL | 32.6371 mL | |
| 5 mM | 0.6527 mL | 3.2637 mL | 6.5274 mL | |
| 10 mM | 0.3264 mL | 1.6319 mL | 3.2637 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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