Eupatilin (Synonyms: NSC 122413) |
| Catalog No.GN10511 |
Eupatilin is a natural flavonoid compound with multiple biological activities. It is an agonist of peroxisome proliferator-activated receptor α (PPARα) and has anti-apoptotic, antioxidant, and anti-inflammatory effects.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 22368-21-4
Sample solution is provided at 25 µL, 10mM.
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Eupatilin is a natural flavonoid compound with multiple biological activities. It is an agonist of peroxisome proliferator-activated receptor α (PPARα) and has anti-apoptotic, antioxidant, and anti-inflammatory effects[1, 2]. Eupatilin has a significant effect in inhibiting tumor growth and can be used in cancer research[3].
In vitro, pretreatment of retinal pigment epithelial (RPE) cells (ARPE-19 cells) with Eupatilin (10, 25, 50μM) for 24h reduced the generation of intracellular ROS induced by H2O2 in a dose-dependent manner, upregulated the expression of Bcl-2 and the phosphorylation levels of PI3K and Akt, downregulated the expression of Bax, and inhibited the activity of caspase-3[4]. Eupatilin (0-400µg/mL) treated osteosarcoma U-2 cells for 96h inhibited cell growth in a dose- and time-dependent manner, changed cell cycle distribution, induced cell apoptosis, induced mitochondrial dysfunction and cytochrome c release[5]. Eupatilin (0-100μM) treated human endometrial cancer cell lines (Hec1A and KLE cells) for 96h significantly inhibited cell viability, was more effective than cisplatin, and induced cell cycle G2/M phase arrest[6].
In vivo, oral treatment of mice treated with transient middle cerebral artery occlusion/reperfusion (tMCAO) surgery with Eupatilin (10mg/kg) significantly reduced cerebral infarction and improved neurological function in tMCAO-challenged mice[7]. Oral treatment of mice with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced Parkinson's disease (PD) with Eupatilin (10mg/kg) for 6 days improved the mice's motor deficits and reduced neuronal loss, inhibiting neuroinflammation and apoptosis[8].
References:
[1] Zeng J, Bao T, Yang K, et al. The mechanism of microglia-mediated immune inflammation in ischemic stroke and the role of natural botanical components in regulating microglia: A review[J]. Frontiers in immunology, 2023, 13: 1047550.
[2] Mavrogonatou E, Kletsas D. Plant-Derived Senotherapeutics for the Prevention and Treatment of Intervertebral Disc Degeneration and Aging[J]. Metabolites, 2024, 14(3): 146.
[3] Wang Y, Hou H, Li M, et al. Anticancer effect of eupatilin on glioma cells through inhibition of the Notch-1 signaling pathway[J]. Molecular Medicine Reports, 2016, 13(2): 1141-1146.
[4] Du L, Chen J, Xing Y. Eupatilin prevents H2O2-induced oxidative stress and apoptosis in human retinal pigment epithelial cells[J]. Biomedicine & Pharmacotherapy, 2017, 85: 136-140.
[5] Li Y Y, Wu H, Dong Y G, et al. Application of eupatilin in the treatment of osteosarcoma[J]. Oncology Letters, 2015, 10(4): 2505-2510.
[6] Cho J H, Lee J G, Yang Y I, et al. Eupatilin, a dietary flavonoid, induces G2/M cell cycle arrest in human endometrial cancer cells[J]. Food and Chemical Toxicology, 2011, 49(8): 1737-1744.
[7] Sapkota A, Gaire B P, Cho K S, et al. Eupatilin exerts neuroprotective effects in mice with transient focal cerebral ischemia by reducing microglial activation[J]. PLoS One, 2017, 12(2): e0171479.
[8] Zhang Y, Qin L, Xie J, et al. Eupatilin prevents behavioral deficits and dopaminergic neuron degeneration in a Parkinson's disease mouse model[J]. Life sciences, 2020, 253: 117745.
| Cell experiment [1]: | |
Cell lines | ARPE-19 cells |
Preparation Method | After reaching 80% confluence, ARPE-19 cells were seeded at a density of 1×105 cells/well in 96-well culture plates and then incubated with different concentrations of Eupatilin (10, 25, and 50μM). Subsequently, the medium was removed, and the cells were exposed to 500μM H2O2 for 24h. The production of ROS was detected by DCFH-DA. |
Reaction Conditions | 10, 25, 50μM; 24h |
Applications | Pretreatment with Eupatilin obviously inhibited ROS production in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male ICR mice |
Preparation Method | Mice that were challenged with transient middle cerebral artery occlusion/reperfusion (tMCAO) were randomly divided into the vehicle-treated, the Eupatilin-treated, or the Edaravone-treated groups. Eupatilin or Edaravone was dissolved in 10% Tween 80 (vehicle). Each group was administered vehicle (10% Tween 80, p.o.), Eupatilin (1, 3, 10mg/kg, p.o.), or Edaravone (3mg/kg, p.o.) immediately after reperfusion. Alternatively, Eupatilin (10mg/kg) was orally administered to mice 5h after MCAO induction. After tMCAO challenge, mice were housed 3 per cage with moist food and soft bedding materials to reduce suffering. Mice were monitored by visual inspection and body weight measurement every 12h following tMCAO till the experimental endpoints. |
Dosage form | 10mg/kg; p.o. |
Applications | Oral administration of Eupatilin (10mg/kg) in a therapeutic paradigm significantly reduced brain infarction and improved neurological functions in tMCAO-challenged mice. |
References: | |
| Cas No. | 22368-21-4 | SDF | |
| Synonyms | NSC 122413 | ||
| Chemical Name | 2-(3,4-dimethoxyphenyl)-5,7-dihydroxy-6-methoxychromen-4-one | ||
| Canonical SMILES | COC1=C(C=C(C=C1)C2=CC(=O)C3=C(C(=C(C=C3O2)O)OC)O)OC | ||
| Formula | C18H16O7 | M.Wt | 344.32 |
| Solubility | ≥ 34.4mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9043 mL | 14.5214 mL | 29.0428 mL |
| 5 mM | 0.5809 mL | 2.9043 mL | 5.8086 mL |
| 10 mM | 0.2904 mL | 1.4521 mL | 2.9043 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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