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    Eupatilin
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    CAS No. 22368-21-4 Price $68 / 20mg
    Catalog No.CFN90190Purity>=98%
    Molecular Weight344.31Type of CompoundFlavonoids
    FormulaC18H16O7Physical DescriptionYellow powder
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    Eupatilin

    Eupatilin
    Product Name Eupatilin
    CAS No.: 22368-21-4
    Catalog No.: CFN90190
    Molecular Formula: C18H16O7
    Molecular Weight: 344.31 g/mol
    Purity: >=98%
    Type of Compound: Flavonoids
    Physical Desc.: Yellow powder
    Targets: TNF-伪 | p65 | NF-kB | IL Receptor | STAT | MAPK | NOS | Bcl-2/Bax | Caspase | Akt | ERK | MMP(e.g.TIMP) | Wnt/尾-catenin | GSK-3
    Source: The leaves of Artemisia argyi Levl.et Vant.
    Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
    Price: $68 / 20mg
    Inquire / Order: manager@chemfaces.com
    Technical Inquiries: service@chemfaces.com
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  • J Mater Chem B.2019, 7(39):5896-5919
  • Planta Med.2016, 82(13):1208-16
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  • HortTechnology2016, 26(6):816-819
  • Phytomedicine.2015, 22(4):498-503
  • Inflammation.2021, doi: 10.1007
  • Int J Mol Sci.2020, 21(19):7209.
  • Nat Prod Sci.2019, 25(3):238
  • Related Screening Libraries
    Size /Price /Stock 10 mM * 100 uL in DMSO / Inquiry / In-stock
    10 mM * 1 mL in DMSO / Inquiry / In-stock
    Related Libraries
  • Hepatoprotective Compound Library
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  • GSK-3 Inhibitor Library
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  • Bcl-2/Bax Inhibitor Library
  • Akt Inhibitor Library
  • Biological Activity
    Description: Eupatilin has anti-inflammatory, and anti-tumor properties, it inhibits the MKN-1 gastric cancer cell proliferation via activation of caspase-3 and the metastatic potential of gastric cancer cells via down-regulation of NF-κB activity followed by reduction of pro-inflammatory cytokine-mediated MMPs expressions. Eupatilin inhibits the signalling of MAPK, IKK, NF-κB and eotaxin-1 in bronchial epithelial cells, leading to inhibition of eosinophil migration. Eupatilin is also a promising therapeutic agent against acute ischemia-induced renal damage, it significantly increases the levels of heat shock protein 70 and B-cell lymphoma protein, and it attenuates inducible nitric oxide synthase, Bcl-2-associated X protein, and caspase-3 levels.
    Targets: TNF-α | p65 | NF-kB | IL Receptor | STAT | MAPK | NOS | Bcl-2/Bax | Caspase | Akt | ERK | MMP(e.g.TIMP) | Wnt/β-catenin | GSK-3
    In vitro:
    Korean J Physiol Pharmacol. 2014 Oct;18(5):383-90.
    The effects of eupatilin (stillen®) on motility of human lower gastrointestinal tracts.[Pubmed: 25352757]
    Gastrointestinal motility consists of phasic slow-wave contractions and the migrating motor complex (MMC). Eupatilin (Stillen®) has been widely used to treat gastritis and peptic ulcers, and various cytokines and neuropeptides are thought to be involved, which can affect gastrointestinal motility.
    METHODS AND RESULTS:
    We performed a study to identify the effects of Eupatilin on lower gastrointestinal motility with electromechanical recordings of smooth muscles in the human ileum and colon. Ileum and colon samples were obtained from patients undergoing bowel resection. The tissues were immediately stored in oxygenated Krebs-Ringer's bicarbonate solution, and conventional microelectrode recordings from muscle cells and tension recordings from muscle strips and ileal or colonic segments were performed. Eupatilin was perfused into the tissue chamber, and changes in membrane potentials and contractions were measured. Hyperpolarization of resting membrane potential (RMP) was observed after administration of Eupatilin. The amplitude, AUC, and frequency of tension recordings from circular and longitudinal smooth muscle strips and bowel segments of the ileum and colon were significantly decreased after admission of Eupatilin. Eupatilin elicited dose-dependent decreases during segmental tension recordings.
    CONCLUSIONS:
    In conclusion, Eupatilin (Stillen®) showed inhibitory effects on the human ileum and colon. We propose that this drug may be useful for treating diseases that increase bowel motility, but further studies are necessary.
    Tumour Biol. 2013 Apr;34(2):875-85.
    Inhibitory effects of eupatilin on tumor invasion of human gastric cancer MKN-1 cells.[Pubmed: 23292941]
    Extracts of the whole herb of Artemisia asiatica Nakai (Asteraceae) are used in traditional oriental medicine to treat inflammation. Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is one of the pharmacologically active components found in A. asiatica, and has been shown to possess anti-tumoral effects in some malignancies, including gastric cancer. However, its anti-metastatic effect in gastric cancer is hardly known.
    METHODS AND RESULTS:
    In this study, anti-metastatic effect of Eupatilin was investigated in the human gastric cancer cell line, MKN-1. Eupatilin inhibited MKN-1 growth in a dose- and a time-dependent manner, and induced apoptosis with a concomitant increase of caspase-3 activity. ELISA demonstrated that release of pro-inflammatory cytokines (IL-1β, TNF-α, IL-6, and IL-8) was significantly reduced by Eupatilin. And p-AKT and p-ERK (p44/42) was reduced. Expression level of β-catenin and integrin was reduced and p-GSKβ was increased. In transcription reporter system, the activity of the transcriptional factor, NF-κB, was reduced by Eupatilin and the expression of p65 was down-regulated when MKN-1 cells were treated with Eupatilin. Moreover, a zymography study revealed that this reduction in invasive potential resulted from a reduction in type IV collagenolytic (gelatinolytic) activity. The expressions of metalloproteinases (MMP-2 and MMP-9) were also reduced in MKN-1 cells treated with Eupatilin. In vitro invasion assay, Eupatilin inhibited MKN-1 penetrating reconstituted basement membrane barriers.
    CONCLUSIONS:
    These results suggest that Eupatilin inhibits the MKN-1 gastric cancer cell proliferation via activation of caspase-3 and the metastatic potential of gastric cancer cells via down-regulation of NF-κB activity followed by reduction of pro-inflammatory cytokine-mediated MMPs expressions.
    In vivo:
    J Korean Med Sci. 2015 Mar;30(3):233-9.
    Eupatilin ameliorates collagen induced arthritis.[Pubmed: 25729243]
    Eupatilin is the main active component of DA-9601, an extract from Artemisia. Recently, Eupatilin was reported to have anti-inflammatory properties. We investigated the anti-arthritic effect of Eupatilin in a murine arthritis model and human rheumatoid synoviocytes.
    METHODS AND RESULTS:
    DA-9601 was injected into collagen-induced arthritis (CIA) mice. Arthritis score was regularly evaluated. Mouse monocytes were differentiated into osteoclasts when Eupatilin was added simultaneously. Osteoclasts were stained with tartrate-resistant acid phosphatase and then manually counted. Rheumatoid synoviocytes were stimulated with TNF-α and then treated with Eupatilin, and the levels of IL-6 and IL-1β mRNA expression in synoviocytes were measured by RT-PCR. Intraperitoneal injection of DA-9601 reduced arthritis scores in CIA mice. TNF-α treatment of synoviocytes increased the expression of IL-6 and IL-1β mRNAs, which was inhibited by Eupatilin. Eupatilin decreased the number of osteoclasts in a concentration dependent manner.
    CONCLUSIONS:
    These findings, showing that Eupatilin and DA-9601 inhibited the expression of inflammatory cytokines and the differentiation of osteoclasts, suggest that Eupatilin and DA-9601 is a candidate anti-inflammatory agent.
    Eupatilin Description
    Source: The leaves of Artemisia argyi Levl.et Vant.
    Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
    Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com

    After receiving: The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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    Calculate Dilution Ratios(Only for Reference)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.9044 mL 14.5218 mL 29.0436 mL 58.0872 mL 72.609 mL
    5 mM 0.5809 mL 2.9044 mL 5.8087 mL 11.6174 mL 14.5218 mL
    10 mM 0.2904 mL 1.4522 mL 2.9044 mL 5.8087 mL 7.2609 mL
    50 mM 0.0581 mL 0.2904 mL 0.5809 mL 1.1617 mL 1.4522 mL
    100 mM 0.029 mL 0.1452 mL 0.2904 mL 0.5809 mL 0.7261 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    Protocol
    Kinase Assay:
    Scand J Immunol. 2015 Mar;81(3):166-76.
    The flavone eupatilin inhibits eotaxin expression in an NF-κB-dependent and STAT6-independent manner.[Pubmed: 25565108]
    The CC chemokine eotaxin contributes to epithelium-induced inflammation in airway diseases such as asthma. Eupatilin (5,7-dihydroxy-3',4',6'-trimethoxyflavone), a bioactive component of Artemisia asiatica Nakai (Asteraceae), is reported to inhibit the adhesion of eosinophils to bronchial epithelial cells. However, little is known about the molecular mechanism of Eupatilin-induced attenuation of bronchial epithelium-induced inflammation.
    METHODS AND RESULTS:
    In this study, we investigated the effect of Eupatilin on expression of eotaxin-1 (CCL11), a potent chemoattractant for eosinophils. Eupatilin significantly inhibited eotaxin expression in bronchial epithelial cells stimulated with TNF-α, while NF-κB and IκBα kinase (IKK) activities declined concurrently. Eupatilin also inhibited mitogen-activated protein kinase (MAPK) activity; however, all of these anti-inflammatory activities were reversed by MAPK overexpression. In contrast, Eupatilin did not affect the signal transducer and activator of transcription 6 (STAT6) signalling in bronchial epithelial cells stimulated with IL-4. Furthermore, Eupatilin significantly attenuated TNF-α-induced eosinophil migration.
    CONCLUSIONS:
    These results suggest that the Eupatilin inhibits the signalling of MAPK, IKK, NF-κB and eotaxin-1 in bronchial epithelial cells, leading to inhibition of eosinophil migration.
    Animal Research:
    Transplant Proc. 2015 Apr;47(3):757-62.
    Protective effect of eupatilin against renal ischemia-reperfusion injury in mice.[Pubmed: 25891726]
    Eupatilin, a pharmacologically active flavone derived from Artemisia species, is known to have antioxidant and anti-inflammatory activities. Ischemia-reperfusion injury (IRI) is a major complication after renal transplantation, with inflammatory responses to IRI exacerbating the resultant renal injury. In the present study, we investigated whether Eupatilin exhibits renoprotective activities against ischemia-reperfusion-induced acute kidney injury in mice.
    METHODS AND RESULTS:
    Renal IRI was induced in male C57BL/6 mice by bilateral renal pedicle occlusion for 30 minutes followed by reperfusion for 48 hours. Eupatilin (10 mg/kg body weight p.o.) was administered 4 days before IRI. Treatment with Eupatilin significantly decreased neutrophil gelatinase-associated lipocalin and kidney injury molecule-1 levels in urine, blood urea nitrogen level, and serum creatinine levels, as well as kidney tubular injury. Western blotting indicated that Eupatilin significantly increased the levels of heat shock protein 70 and B-cell lymphoma protein, and it attenuated inducible nitric oxide synthase, Bcl-2-associated X protein, and caspase-3 levels 48 hours after IRI.
    CONCLUSIONS:
    Our findings suggest that Eupatilin is a promising therapeutic agent against acute ischemia-induced renal damage.
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