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    Baicalein
    Baicalein

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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 #: V0807
    CAS #: 491-67-8Purity ≥98%

    Description: Baicalein (5,6,7-Trihydroxyflavone; Noroxylin; BaiKalein), a naturally occuring flavone, is a potent inhibitor of CYP2C9, prolyl endopeptidase, and xanthine oxidase with important biological activity (e.g, antioxidant, anti-inflammation, antifibrotic). Baicalin can be isolated from several species in the genus Scutellaria, including Scutellaria lateriflora (blue skullcap). There are 10 mg/g baicalin in Scutellaria galericulata (common skullcap) leaves. Baicalin is the glucuronide of baicalein. It is a component of Chinese medicinal herb Huang-chin (Scutellaria baicalensis) and one of the chemical ingredients of Sho-Saiko-To, an herbal supplement. Baicalin is a known prolyl endopeptidase inhibitor, induces apoptosis in pancreatic cancer cells, and affects the GABA receptors. 

    References: Drug Metab Dispos. 2009 Mar;37(3):629-34.


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    Molecular Weight (MW)270.24
    FormulaC15H10O5
    CAS No.491-67-8
    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
    Other info

    Chemical Name: 5,6,7-Trihydroxy-2-phenylchromen-4-one

    InChi Key: FXNFHKRTJBSTCS-UHFFFAOYSA-N

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

    SMILES Code: O=C1C=C(C2=CC=CC=C2)OC3=C1C(O)=C(O)C(O)=C3

    SynonymsNoroxylin; 5,6,7-Trihydroxyflavone; Baicalein; BaiKalein;


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    In Vitro

    In vitro activity: Baicalein suppresses mitogen induced T cell proliferation and cytokine secretion in vitro. Pre-treatment with baicalein significantly suppresses Con A or anti-CD3/CD28 mAb induced proliferation as well as cytokine secretion at 25 μM. Baicalein treatment induces DNA binding of NF-κB but inhibits thioredoxin activity in the nuclear compartment. Baicalein suppresses proliferation, migration, and invasion of MDA-MB-231 cells in a time- and dose-dependent manner. Baicalein significantly decreases the expression of SATB1 in MDA-MB-231 cells. Baicalein also downregulates the expression of Wnt1 and β-catenin proteins and transcription level of Wnt/β-catenin-targeted genes.


    Cell Assay: MTT assay is conducted to evaluate the effect of baicalein on proliferation of breast cancer cells. MDA-MB-231 cells are routinely digested, collected, and then seeded in 96-well plates at a density of 8×103 cells/well. After incubation for 12-24 hours, cells are treated with 0, 20, 40, 60, 80, 100, and 120 μM baicalein according to their experimental grouping and then incubated at 37°C for 24, 48, and 72 hours.

    In VivoBaicalein suppresses induction of graft versus host disease but does not inhibit homeostatic proliferation of T-cells in mice. This observation clearly shows potent anti-inflammatory activity of baicalein in vivo. Rats treated with baicalein are protected against an increase in heart to body weight ratio, plasma level of brain natriuretic peptides, intraventricular septum thickness, myocardial collagen volume of left ventricle (all P<0.05, respectively). The antifibrotic effects of baicalein are further illustrated by the suppressed expression of left ventricle pro-collagens I and III accompanied by the decreased expression of 12-lipoxygenase, and by reduced expression and activity of matrix metallopeptidase 9 and extracellular signal-regulated kinases. Baicalein can inhibit cardiac fibrosis in hypertensive rats.
    Animal modelRats and mice
    Formulation & Dosage

    Rats: Baicalein is suspended in 1% methylcellulose. Rats are treated with baicalein suspension via oral garvage. SHR and WKY rats are divided into 4 groups (n=8 per group): 12-week treatment with high-dose (200 mg/kg/day) or low-dose (50 mg/kg/day) group; and 4-week treatment with high-dose or low-dose group. The 12-week and 4-week negative control groups of SHR and WKY rats (n=8 per group) receive vehicle while positive control groups (Val group, n=8 per group) receive valsartan (20 mg/kg/day) for comparison[4].

    Mice: To study the in vivo anti-inflammatory efficacy of baicalein, graft-versus-host disease (GVHD) model is used. Splenic lymphocytes from C57BL/6 mice are incubated with baicalein in vitro (25 μM, 4h) and adoptively transferred to immune-compromised Balb/c mice.

    References

    [1]. Shieh DE,et al. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res. 2000 Sep-Oct;20(5A):2861-5.

    [2]. Patwardhan RS, et al. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation. Biochem Pharmacol. 2016 May 15;108:75-89.

    [3]. Ma X, et al. Baicalein suppresses metastasis of breast cancer cells by inhibiting EMT via downregulation of SATB1 and Wnt/β-catenin pathway. Drug Des Devel Ther. 2016 Apr 18;10:1419-41.

    [4]. Kong EK, et al. A novel anti-fibrotic agent, baicalein, for the treatment of myocardial fibrosis in spontaneously hypertensiverats. Eur J Pharmacol. 2011 May 11;658(2-3):175-81.


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

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