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    Apigenin
    Apigenin

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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 #: V0808
    CAS #: 520-36-5Purity ≥98%

    Description: Apigenin (NSC-83244, LY-080400; 4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1) is a natural flavonoid acting as a potent P450 inhibitor with various biological activity (e.g, antioxidant, anti-inflammation, anticancer). It inhibits CYP2C9 with Ki of 2 μM. Apigenin is a natural flavonoid product isolated from many plants and belongs to the flavone class that is the aglycone of several naturally occurring glycosides. Apigenin is an antioxidant plant flavanoid which contains anti-inflammatory and anticancer properties. It may induce apoptosis and may inhibit proliferation of tumor cells by arresting the cell cycle at the G2/M phase. 

    References: J Cell Biochem Suppl. 1997;28-29:39-48; Pharm Res. 2010 Jun;27(6):962-78. 

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    Molecular Weight (MW)270.24
    FormulaC15H10O5
    CAS No.520-36-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 54 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)

    Chemical Name: 5,7-Dihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one

    InChi Key: KZNIFHPLKGYRTM-UHFFFAOYSA-N

    InChi Code: InChI=1S/C15H10O5/c16-9-3-1-8(2-4-9)13-7-12(19)15-11(18)5-10(17)6-14(15)20-13/h1-7,16-18H

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

    SynonymsLY080400; NSC-83244, LY-080400; NSC83244, NSC 83244, LY 080400; Apigenine; Chamomile; Apigenol; Spigenin; Versulin; 457Trihydroxyflavone; C.I. Natural Yellow 1


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    In Vitro

    In vitro activity: Apigenin inhibits PKC by competing with adenosine triphosphate (ATP). Apigenin also reduces the level of TPA-stimulated phosphorylation of cellular proteins and inhibits TPA-induced c-jun and c-fos expression. Apigenin exhibits the reverting effect on the transformed morphology of v-H-ras transformed NIH3T3 cells. Apigenin has been shown to possess anti-mutagenic properties in a setting of nitropyrene-induced genotoxicity in Chinese hamster ovary cells. Apigenin suppresses of LPS-induced cyclooxygenase-2 and nitric oxide synthase-2 activity and expression in mouse macrophages. Apigenin has been reported to inhibit protein kinase C activity, mitogen-activated protein kinase (MAPK), transformation of C3HI mouse embryonic fibroblasts and downstream oncogenes in v-Ha-ras-transformed NIH3T3 cells. Apigenin blocks peroxisome proliferation-regulated kinase (ERK), a MAPK in isolated hepatocytes. Apigenin has further been shown to down-regulate the expression of the Na+/Ca2+-exchanger, a protein important for calcium extrusion in neonatal rat cardiac myocytes. Apigenin induces a reversible G2/M and G0/G1 arrest by inhibiting p34 (cdc2) kinase activity, accompanied by increased p53 protein stability in epidermal cells and fibroblasts. Apigenin is also effective in inhibiting TNFα-induced intracellular adhesion molecule-1 upregulation in cultured human endothelial cells. Apigenin inhibits the expression of HIF-1α and VEGF via the PI3K/Akt/p70S6K1 and HDM2/p53 pathways in human ovarian cancer cells. Apigenin inhibits differentiation by suppressing MAPK signal transduction and reducing API transcription factor level in human keratinocytes. Apigenin also inhibits proliferating of human keratinocytes.


    Cell Assay: The effect of Apigenin on the viability of cells is determined by MTT assay. Near-confluent stock cultures of human gastric cancer SGC-7901 cells are harvested with 0.2% EDTA and plated at a density of 2.5×103/well in 96-well microtiter plates. After an overnight incubation to allow cell attachment, the medium is replaced by fresh medium containing different concentrations (0, 20, 40, and 80 μM) of Apigenin. Control wells receive DMSO (0.2%). Each concentration of Apigenin is repeated in four wells. After incubation for 24 h, one plate is assayed with a microplate reader at the wavelength of 570 nm. Before the assay, MTT (5 mg/mL in PBS) is added to each well and incubated for 4 h, then MTT solution is removed from the wells by aspiration. After careful removal of the medium, 0.1 mL of DMSO is added to each well, and the plate is shaken for 15 min. The data of 7 d are fed into the computer and the growth curve is drawn. The growth inhibition rate (IR) is calculated.

    In VivoApigenin down-regulates production of IL-4 in ovalbumin-immunized BALB/C mice. Apigenin inhibits melanoma lung metastases by impairing interaction of tumor cells with endothelium. Apigenin is shown to cause a significant increase in uterine weight and overall uterine concentration of estrogen receptor (ER)-α in female mice (64) and also suppresses prostate and breast cancer cell growth through estrogen receptor β1. Apigenin suppresses the levels of IGF-I in prostate tumor xenografts and increases levels of IGFBP-3, a binding protein that sequesters IGF-I in vascular circulation. Apigenin (12.5 mg/kg) increases cell proliferation in the dentate gyrus of hippocampus of adult mice. 
    Animal modelMice
    Formulation & Dosage12.5 mg/kg
    References

     J Cell Biochem Suppl. 1997;28-29:39-48.; Pharm Res. 2010 Jun;27(6):962-78. 


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

    Apigenin


    The effect of UVB and apigenin on TSP1 expression in epidermal keratinocytes in vitro and in vivo. Oncotarget. 2014 Nov; 5(22): 11413–11427.
     

    Apigenin

    The effect of apigenin and TSP1 peptide mimetic (ABT-898) on UVB-induced skin thickening and proliferation. Oncotarget. 2014 Nov; 5(22): 11413–11427.
     

    Apigenin

    Apigenin regulates TSP1 translation via HuR. Oncotarget. 2014 Nov; 5(22): 11413–11427.


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