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| ln Vitro |
In vitro studies assessed the effect of 12-Epinapelline N-oxide on the functional activity of fibroblast precursors. Bone marrow cells from intact CBA/CaLac mice were cultured, and the compound was added at concentrations of 1, 10, 50, and 100 nM. The number of fibroblast colony‑forming units (CFU‑F) was evaluated. At a concentration of 50 nM, 12-Epinapelline N-oxide significantly increased the number of CFU‑F compared to the basal level. At 100 nM, the compound also significantly stimulated colony growth relative to the basal level. These findings indicate direct, dose‑dependent stimulation of CFU‑F activity by 12-Epinapelline N-oxide. [2]
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| ln Vivo |
In the carrageenan‑induced acute inflammation model (subplantar injection of 0.1 ml 1% carrageenan in albino outbred CD1 mice and CBA mice, 20‑30 g), therapeutic administration of 12-Epinapelline N-oxide (0.025 mg/kg given for 5 days, last dose 1 hour after carrageenan) significantly reduced paw edema by 39% compared to control values. Preventive administration (1 hour before carrageenan) did not produce a significant antiexudative effect. [1]
In the histamine‑induced edema model (subplantar injection of 0.1% histamine), 12-Epinapelline N-oxide (0.025 mg/kg course treatment) contributed to a significant decrease in the exudative reaction, reducing edema by 1.2‑ to 1.8‑fold relative to controls. [1] In the arachidonic acid‑induced inflammation model (subplantar injection of 0.1% arachidonic acid), preventive treatment with 12-Epinapelline N-oxide (0.025 mg/kg) resulted in a 6.3% inhibition of edema (limb weight increment 13.9±2.7% vs. control 15.0±1.7%), which was not statistically significant. [1] In the acetic acid‑induced peritonitis model (intraperitoneal injection of 1% acetic acid), 12-Epinapelline N-oxide (0.025 mg/kg course treatment) significantly reduced the volume of ascitic fluid by 12% (0.38±0.04 ml vs. control 0.43±0.02 ml). [1] |
| Cell Assay |
The fibroblast colony‑forming unit (CFU‑F) culture method was used. Bone marrow cells from intact CBA/CaLac mice were harvested and cultured under conditions promoting fibroblast colony growth. 12-Epinapelline N-oxide was added to the culture medium at concentrations of 1, 10, 50, and 100 nM. After the standard culture period, the cultures were evaluated for colony formation. Fibroblast colonies were defined as cell aggregates containing more than 50 cells. The number of CFU‑F grown from 2.5×10⁵ nucleated cells was counted and compared to the basal level (no alkaloid addition). [2]
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| Animal Protocol |
Anti‑inflammatory activity protocol [1]: Experiments were performed on albino outbred mature CD1 mice and CBA mice weighing 20‑30 g. 12-Epinapelline N-oxide was administered at a dose of 0.025 mg/kg for 5 days (course treatment). The last dose was given either 1 hour before (preventive regimen) or 1 hour after (therapeutic regimen) the induction of inflammation. Acute inflammation was induced by: subplantar injection of 0.1 ml of 1% carrageenan; subplantar injection of 0.1% histamine; subplantar injection of 0.1% arachidonic acid; or intraperitoneal injection of 1% acetic acid to induce peritonitis. After 3 hours, animals were sacrificed, and inflammatory responses were measured by limb weight increment or volume of ascitic fluid.
Ulcerogenic effect evaluation protocol [1]: After treatment, the gastrointestinal tract of mice was examined for mucosal damage. A 4‑point scale was used: 0 = no damage, 0.5 = congestion, 1 = minor single injuries (1‑2 petechial hemorrhages), 2 = multiple injuries (erosions, petechial hemorrhages), 3 = considerable and multiple mucosal injury, 4 = gross lesions covering the entire mucosal surface. A score ≥2 indicates ulcerogenic activity. |
| Toxicity/Toxicokinetics |
The ulcerogenic effect (gastrotoxicity) of 12-Epinapelline N-oxide was evaluated in mice. The compound exhibited an ulcerogenic index score of 0.4±0.2, which is below the threshold of 2, indicating no significant gastric mucosal damage. Specifically, hyperemia score was 0.2±0.2 and hemorrhage score (absolute units) was 0.7±0.5. This suggests that 12-Epinapelline N-oxide does not exert ulcerogenic effects, likely because it does not inhibit constitutive cyclooxygenase (COX‑1) involved in the production of protective prostaglandins. No other toxicity data (e.g., LD₅₀, hepatotoxicity, nephrotoxicity) are reported. [1]
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| References | |
| Additional Infomation |
12-Epinapelline is a coalkyl diterpenoid compound. It has been reported to exist in Aconitum carmichaelii, Aconitum japonicum, and other organisms with relevant data.
12-Epinapelline N-oxide is a diterpene alkaloid of the atisine type isolated from Aconitum baikalense. It exhibits anti‑inflammatory activity comparable to diclofenac sodium in various acute inflammation models, yet unlike non‑steroidal anti‑inflammatory drugs (NSAIDs), it lacks ulcerogenic effects. The mechanism of its anti‑inflammatory action is thought to involve inhibition of the biological effects of inflammatory mediators such as histamine, serotonin, and arachidonic acid, rather than inhibition of prostaglandin synthase. [1] In terms of regenerative properties, 12-Epinapelline N-oxide directly stimulates fibroblast precursors (CFU‑F) in vitro. Since CFU‑F include mesenchymal stem cells (MSC), this stimulation may contribute to more complete tissue regeneration and wound healing when present in complex extracts of Aconitum baikalense. [2] |
| Molecular Formula |
C22H33NO3
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|---|---|
| Molecular Weight |
359.5023
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| Exact Mass |
359.246
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| CAS # |
110064-71-6
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| PubChem CID |
3133561
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
537.8±50.0 °C at 760 mmHg
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| Flash Point |
284.2±28.8 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.638
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| LogP |
0.78
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
26
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| Complexity |
695
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN1CC2(CCC(C34C2CC(C31)C56C4CC(C(C5)C(=C)C6O)O)O)C
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| InChi Key |
AZAZKLKDEOMJBJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H33NO3/c1-4-23-10-20(3)6-5-17(25)22-15(20)7-13(18(22)23)21-9-12(11(2)19(21)26)14(24)8-16(21)22/h12-19,24-26H,2,4-10H2,1,3H3
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| Chemical Name |
11-ethyl-13-methyl-6-methylidene-11-azahexacyclo[7.7.2.15,8.01,10.02,8.013,17]nonadecane-4,7,16-triol
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~278.16 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.95 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7816 mL | 13.9082 mL | 27.8164 mL | |
| 5 mM | 0.5563 mL | 2.7816 mL | 5.5633 mL | |
| 10 mM | 0.2782 mL | 1.3908 mL | 2.7816 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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