Columbin
Based on 1 publication(s) in Google Scholar
Columbin is an orally active diterpenoid furanolactone from Calumbae radix, has anti-inflammatory and anti-trypanosomal effects. Columbin selectively inhibits COX-2 (EC50=53.1 μM) over COX-1 (EC50=327 μM).
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- Pureza: 99.80%
- No. CAS: 546-97-4
- Fòrmula: C20H22O6
- Peso molecular:358.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Columbin
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Actividad biológica
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Trypanosoma |
COX-2 53.1 μM (EC50) |
COX-1 327 μM (EC50) |
Treatment with columbin or l-NAME inhibits LPS/IFN-γ-induced NO production without affecting the viability of RAW264.7. Pre-treatment of stimulated cells with columbin does not inhibit the translocation of NF-κB to the nucleus in LPS-stimulated cells. COX-1 and COX-2 inhibitory activities of columbin are 63.7±6.4% and 18.8±1.5% inhibition at 100μM, respectively. The interaction of columbin with Tyr385 and Arg120 signifies its higher activity in COX-2, as Tyr385 is reported to be involved in the abstraction of hydrogen from C-13 of arachidonate, and Arg120 is critical for high affinity arachidonate binding[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 546-97-4
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Appearance Solid
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Peso molecular 358.39
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Fòrmula C20H22O6
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Color White to off-white
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SMILES
O=C1[C@](C=C2)(O)[C@@](CC3)(C)[C@@]([C@@](C[C@@H](C4=COC=C4)O5)(C)[C@]3([H])C5=O)([H])[C@]2([H])O1
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (279.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (6.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Protocolo
Rats: Male Wistar rats are treated as following: i.v. injection of columbin in EtOH and PEG-300 (1:1) is administrated through tail vein at dose of 20 mg/kg. Intraperitoneal (i.p.) injection of columbin in EtOH and PEG-300 (1:1) is administrated at dose of 20 mg/kg. An oral gavage of columbin suspended in oral suspension vehicle is given to rats at dose of 50 mg/kg. Blood samples (50-100 μL) are collected by snipping the tail into heparinized tubes at 0, 5, 15, 30, 45, 60, 120, 240, 360, 480 and 1440 min for i.v. administration, or at 0, 15, 30, 60,120, 180, 240, 360, 480, 1440 min for oral dosing or i.p. injection. The blood samples are stored at −20°C until analysis[2].
Mice: Male Balb/c mice (n=60) are randomly divided into six groups. Columbin is intra-peritoneally administered to mice at the dose of 30, 100, 300 and 700 mg/kg. Aspirin, an anti-inflammatory drug, is used as a positive control. To induce acute phase inflammation in paw, rats are injected subcutaneously into the right hind paw with a 1% solution of carrageenan dissolved in saline 30 min after vehicle or columbin treatment. The paw volumes are measured up to 5 h after the injection at intervals of 1 h. Paw volume is measured with a plethysmometer immediately prior to the injection of carrageenan and thereafter at an interval of 1 h for a period of 5 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ibrahim Abdelwahab S, et al. In vitro and in vivo anti-inflammatory activities of columbin through the inhibition of cycloxygenase-2 and nitric oxide but not the suppression of NF-κB translocation. Eur J Pharmacol. 2012 Mar 5;678(1-3):61-70. [Content Brief]
[2]. A J Nok, et al. Columbin inhibits cholesterol uptake in bloodstream forms of Trypanosoma brucei-A possible trypanocidal mechanism.J Enzyme Inhib Med Chem. 2005 Aug;20(4):365-8. [Content Brief]
[3]. Yang G, et al. Development and validation of an UPLC-MS/MS method for the quantification of columbin in biological matrices: Applications to absorption, metabolism, and pharmacokinetic studies. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:13-8 [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7903 mL | 13.9513 mL | 27.9026 mL | 69.7564 mL |
| 5 mM | 0.5581 mL | 2.7903 mL | 5.5805 mL | 13.9513 mL | |
| 10 mM | 0.2790 mL | 1.3951 mL | 2.7903 mL | 6.9756 mL | |
| 15 mM | 0.1860 mL | 0.9301 mL | 1.8602 mL | 4.6504 mL | |
| 20 mM | 0.1395 mL | 0.6976 mL | 1.3951 mL | 3.4878 mL | |
| 25 mM | 0.1116 mL | 0.5581 mL | 1.1161 mL | 2.7903 mL | |
| 30 mM | 0.0930 mL | 0.4650 mL | 0.9301 mL | 2.3252 mL | |
| 40 mM | 0.0698 mL | 0.3488 mL | 0.6976 mL | 1.7439 mL | |
| 50 mM | 0.0558 mL | 0.2790 mL | 0.5581 mL | 1.3951 mL | |
| 60 mM | 0.0465 mL | 0.2325 mL | 0.4650 mL | 1.1626 mL | |
| 80 mM | 0.0349 mL | 0.1744 mL | 0.3488 mL | 0.8720 mL | |
| 100 mM | 0.0279 mL | 0.1395 mL | 0.2790 mL | 0.6976 mL |
Columbin Related Classifications
HY-N0389 Related Classifications
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