| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Britannin targets multiple signaling pathways involved in inflammation and cancer. Its primary mechanism involves the activation of AMPK (AMP-activated protein kinase) regulated by ROS (reactive oxygen species). By activating AMPK, Britannin induces apoptosis and autophagy in cancer cells. The compound also inhibits the activation of NF-κB and MAPK, leading to the suppression of LPS-induced nitric oxide, PGE2, and cytokine production. Britannin induces apoptosis through the mitochondrial pathway, as demonstrated by its effects on MCF-7 and MDA-MB-468 breast cancer cells. The compound's anti-proliferative effects are mediated through the activation of the mitochondrial apoptotic pathway. Through these mechanisms, Britannin exerts anti-inflammatory, anti-proliferative, and pro-apoptotic effects.
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| ln Vitro |
In vitro, Britannin has been shown to inhibit the growth of various cancer cell lines and induce apoptosis. The compound induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin exhibits anti-proliferative activity on MCF-7 and MDA-MB-468 human breast cancer cells through the activation of the mitochondrial apoptotic pathway. The compound suppresses LPS-induced nitric oxide, PGE2, and cytokine production via NF-κB and MAPK inactivation in RAW 264.7 macrophages. The compound's effects on cell viability, apoptosis, autophagy, and inflammatory marker expression can be assessed in various cell culture systems. Britannin has anti-proliferative and anti-inflammatory activities.
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| ln Vivo |
In vivo, Britannin has been studied in animal models for its anti-tumor and anti-inflammatory effects. The compound's ability to induce apoptosis and autophagy through AMPK activation suggests potential anti-tumor efficacy in vivo. Its anti-inflammatory effects, mediated through NF-κB and MAPK inactivation, indicate potential benefits in inflammatory conditions. However, detailed in vivo studies are needed to fully characterize the compound's efficacy, pharmacokinetics, and safety profile. The compound's therapeutic potential in liver cancer and other malignancies is an area of active research.
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| Enzyme Assay |
For non-cellular enzyme assays, Britannin can be tested for inhibition of kinases such as AMPK, MAPK, and other signaling molecules using standard kinase activity assays. The compound's ability to modulate NF-κB activity can be assessed using electrophoretic mobility shift assays (EMSA) or luciferase reporter assays with purified components. The compound's antioxidant activity can be evaluated using cell-free assays such as DPPH, ABTS, or FRAP radical scavenging assays. The compound's binding affinity to its molecular targets can be assessed using surface plasmon resonance or other biophysical techniques.
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| Cell Assay |
For in vitro cell-based assays, cancer cell lines (such as liver cancer cells, MCF-7, and MDA-MB-468 breast cancer cells) and inflammatory cell models (such as RAW 264.7 macrophages) are cultured and treated with Britannin. Cell proliferation is assessed using MTT or CCK-8 assays. Apoptosis is evaluated by flow cytometry using Annexin V/PI staining or by assessing caspase activity. Autophagy is assessed by measuring LC3-II levels and autophagosome formation. Inflammatory marker expression (nitric oxide, PGE2, cytokines) is measured by ELISA or Griess assay. Signaling pathway activation (AMPK, NF-κB, MAPK) is assessed using Western blotting with phospho-specific antibodies.
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| Animal Protocol |
For in vivo animal studies, Britannin can be administered to animal models of disease. In cancer models, the compound can be evaluated in xenograft models of liver cancer or breast cancer, where tumor growth, apoptosis markers, autophagy markers, and survival are assessed. In inflammation models, the compound can be tested in models of acute or chronic inflammation, such as LPS-induced endotoxemia or carrageenan-induced paw edema. Pharmacokinetic and pharmacodynamic studies can be performed to characterize the compound's absorption, distribution, metabolism, and excretion.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Britannin include a molecular weight of 366.41 and a molecular formula of C₁₈H₂₆O₇. The compound is soluble in DMSO at 250 mg/mL (682.30 mM). The compound should be stored at 4°C, protected from light. Stock solutions can be stored below -20°C for several months. For obtaining a higher solubility, the tube should be warmed at 37°C and shaken in an ultrasonic bath. The compound is shipped with blue ice for evaluation sample solutions, or at room temperature for other sizes.
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| Toxicity/Toxicokinetics |
As a natural product, Britannin is generally considered safe at low doses. No significant toxicity has been reported in preclinical studies. However, comprehensive toxicological evaluations are needed to establish the compound's safety for potential therapeutic use. The compound is intended for research use only and is not for human use.
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| References |
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| Additional Infomation |
From Inula aucheriana; see the first source for structure.
Britannin is a naturally occurring sesquiterpene lactone found in Inula aucheriana, Inula caspica, and other Asteraceae plants. It induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. The compound exhibits anti-proliferative activity on MCF-7 and MDA-MB-468 breast cancer cells through the activation of the mitochondrial apoptotic pathway. Britannin suppresses LPS-induced nitric oxide, PGE2, and cytokine production via NF-κB and MAPK inactivation. The compound has anti-proliferative and anti-inflammatory activities. It is not currently approved for clinical use and is available only for research purposes. |
| Molecular Formula |
C19H26O7
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|---|---|
| Molecular Weight |
366.40554
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| Exact Mass |
366.168
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| CAS # |
33627-28-0
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| PubChem CID |
14466541
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| Appearance |
White to off-white solid powder
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| Density |
1.25±0.1 g/cm3
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| Melting Point |
189-191 ºC
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| LogP |
1.374
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
656
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@@H]1C[C@H]2[C@H]([C@@H]([C@]3([C@H]1[C@H](C[C@@H]3O)OC(=O)C)C)OC(=O)C)C(=C)C(=O)O2
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| InChi Key |
JXEGMONJOSAULB-IZZBGLMFSA-N
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| InChi Code |
InChI=1S/C19H26O7/c1-8-6-12-15(9(2)18(23)26-12)17(25-11(4)21)19(5)14(22)7-13(16(8)19)24-10(3)20/h8,12-17,22H,2,6-7H2,1,3-5H3/t8-,12+,13+,14+,15-,16-,17+,19-/m1/s1
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| Chemical Name |
[(3aS,5R,5aS,6S,8S,8aS,9S,9aR)-9-acetyloxy-8-hydroxy-5,8a-dimethyl-1-methylidene-2-oxo-4,5,5a,6,7,8,9,9a-octahydro-3aH-azuleno[6,5-b]furan-6-yl] acetate
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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 : ~250 mg/mL (~682.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.68 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 (5.68 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 (5.68 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 | 2.7292 mL | 13.6459 mL | 27.2918 mL | |
| 5 mM | 0.5458 mL | 2.7292 mL | 5.4584 mL | |
| 10 mM | 0.2729 mL | 1.3646 mL | 2.7292 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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