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    Diosmetin
    Diosmetin

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0810
    CAS #: 520-34-3Purity ≥98%

    Description: Diosmetin (also known as DIO; HSDB 8101; HSDB 8101; Luteolin 4'-methyl ether) is a naturally occuring flavonoid found in spearmint, oregano, and many other plants with various biological activity (e.g, antioxidant, anti-inflammation, anticancer). It inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell. Diosmetin is also an agonist of the aryl hydrocarbon receptor (AHR). It potently inhibited the enzyme activity of cytochrome P450 1A1 (CYP1A1) in a dose-dependent manner with an IC50 value of approximately 30 nM, in microsomes from MCF-7 cells.

    References: Pharmacol Res. 1992 Dec;26(4):395-402; Cancer Res. 1998 Jul 1;58(13):2754-60.

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    Molecular Weight (MW)300.26
    FormulaC16H12O6
    CAS No.520-34-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 60 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)

    Chemical Name: 5,7-dihydroxy-2-(3-hydroxy-4-methoxyphenyl)-4H-chromen-4-one

    InChi Key: MBNGWHIJMBWFHU-UHFFFAOYSA-N

    InChi Code: InChI=1S/C16H12O6/c1-21-13-3-2-8(4-10(13)18)14-7-12(20)16-11(19)5-9(17)6-15(16)22-14/h2-7,17-19H,1H3

    SMILES Code: O=C1C=C(C2=CC=C(OC)C(O)=C2)OC3=CC(O)=CC(O)=C13           

    SynonymsLuteolin 4-methyl ether; HSDB-8101; Diosmetin; HSDB 8101; HSDB 8101; Luteolin 4'-methyl ether


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    In Vitro

    In vitro activity: Diosmetin inhibits 3H-dopamine uptake in neuroblastoma cells, as well as in small-cell lung carcinoma cells, which is be responsible for the increased vascular tone observed in vivo after treatment with Diosmetin. Moreover, Diosmetin also removes iron from iron-loaded hepatocytes revealed a good relationship between this iron-chelating ability and the cytoprotective effect. Other studies proves that Diosmetin is a cytochrome P450 inhibitor, thus inhibiting carcinogen activation and and causing pharmacokinetic interactions with co-administered drugs metabolized.


    Cell Assay: In MCF-7 cells, at 24 h after the incubation of diosmetin, CYP1A1 mRNA was increased in a dose-dependent manner. In MCF-7 cells, diosmetin at 2.5 µM modestly increased CYP1A1 enzyme activity, with an activity increase in cells, while diosmetin at 5 µM did not increase the enzyme activity compared to controls in cells. Compared with controls, diosmetin dose-dependently increased the capacity of nuclear extracts to bind an oligonucleotide containing the AhR-binding sequence of CYP1A1.

    In VivoPretreatment with diosmetin significantly reduces serum levels of amylase and lipase; the histological injury; the secretion of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6; myeloperoxidase (MPO) activity, trypsinogen activation peptide (TAP) level, the expression of inducible nitric oxide synthase (iNOS); and the nuclear factor (NF)-κB activation in cerulein-induced acute pancreatitis.
    Animal modelMice: Experimental acute pancreatitis is induced in mice by seven intraperitoneal injection of cerulein (50 μg/kg) at hourly intervals. Diosmetin (100 mg/kg) or vehicle is pretreated 2 h before the first cerulein injection. After 6 h, 9 h, 12 h of the first cerulein injection, the severity of acute pancreatitis is evaluated biochemically and morphologically
    Formulation & Dosage100 mg/kg
    References

    Pharmacol Res. 1992 Dec;26(4):395-402; Cancer Res. 1998 Jul 1;58(13):2754-60.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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