Leonuriside A
Based on 1 Customer Validation
Leonuriside A is a phenolic compound that can be isolated from Leonurus japonicus. Leonuriside A exhibits anti-inflammatory activity, which inhibits the iNOS-related inflammatory pathway in LPS (HY-D1056)-stimulated macrophages, thereby suppressing the production of nitric oxide (NO) with an IC50 of 15.6 μM. Leonuriside A can be used in studies of anti-inflammatory natural products and the molecular mechanisms of inflammation.
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- Pureté : 99.79%
- CAS No.: 121748-12-7
- Formule: C14H20O9
- Masse moléculaire:332.30
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Description
IC50 & Target
[1]|
iNOS |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
15.6 μM
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Inhibition of nitric oxide production in LPS-stimulated RAW264.7 macrophages assessed via Griess method after 30 min pretreatment with Leonuriside A followed by 24 h incubation with LPS.
Inhibition of nitric oxide production in LPS-stimulated RAW264.7 macrophages assessed via Griess method after 30 min pretreatment with Leonuriside A followed by 24 h incubation with LPS.
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7416973 |
In Vitro
Leonuriside A (up to 50 μM; 30 min pretreatment, 24 h LPS incubation) inhibits nitric oxide production in LPS-stimulated RAW264.7 macrophages with an IC50 of 15.6 μM, with no significant cytotoxicity at concentrations up to 50 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 121748-12-7
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Appearance Solid
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Masse moléculaire 332.30
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Formule C14H20O9
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Color White to off-white
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SMILES
O[C@H]([C@H]([C@@H]([C@@H](CO)O1)O)O)[C@@H]1OC2=C(OC)C=C(O)C=C2OC
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (300.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (15.05 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (15.05 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cotton Pellet Granuloma
Cotton pellet granuloma is a classical in vivo chronic inflammation model used to evaluate the anti-inflammatory potential of test substances by measuring their ability to inhibit granuloma tissue formation around an implanted foreign body (cotton pellet) in rodents. The method is based on the biological response to a sterile implanted material, which induces proliferative phase inflammation characterized by fibroblast proliferation and collagen-rich granuloma formation, and the final readout reflects the extent of chronic inflammatory tissue growth surrounding the pellet. In multiple preclinical pharmacological evaluations, inhibition of cotton pellet-induced granuloma formation has been used as an indicator of anti-inflammatory activity in both synthetic and natural product screening contexts.
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
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Fiche technique (291 KB)
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SDS (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ba Vinh L, et al. Bioactive triterpene glycosides from the fruit of Stauntonia hexaphylla and insights into the molecular mechanism of its inflammatory effects. Bioorganic & medicinal chemistry letters. 2019 Aug 15;29(16):2085-2089. [Content Brief]
[3]. Minh TT. et al. Lignans from the stems of Clerodendrum inerme Gaertn. VJCH, 59: 187-191.
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0093 mL | 15.0466 mL | 30.0933 mL | 75.2332 mL |
| 5 mM | 0.6019 mL | 3.0093 mL | 6.0187 mL | 15.0466 mL | |
| 10 mM | 0.3009 mL | 1.5047 mL | 3.0093 mL | 7.5233 mL | |
| 15 mM | 0.2006 mL | 1.0031 mL | 2.0062 mL | 5.0155 mL | |
| 20 mM | 0.1505 mL | 0.7523 mL | 1.5047 mL | 3.7617 mL | |
| 25 mM | 0.1204 mL | 0.6019 mL | 1.2037 mL | 3.0093 mL | |
| 30 mM | 0.1003 mL | 0.5016 mL | 1.0031 mL | 2.5078 mL | |
| 40 mM | 0.0752 mL | 0.3762 mL | 0.7523 mL | 1.8808 mL | |
| 50 mM | 0.0602 mL | 0.3009 mL | 0.6019 mL | 1.5047 mL | |
| 60 mM | 0.0502 mL | 0.2508 mL | 0.5016 mL | 1.2539 mL | |
| 80 mM | 0.0376 mL | 0.1881 mL | 0.3762 mL | 0.9404 mL | |
| 100 mM | 0.0301 mL | 0.1505 mL | 0.3009 mL | 0.7523 mL |