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    Imperatorin
    Information
    CAS No. 482-44-0 Price $40 / 20mg
    Catalog No.CFN98758Purity>=98%
    Molecular Weight270.3 Type of CompoundCoumarins
    FormulaC16H14O4Physical DescriptionCryst.
    Download Manual    COA    MSDSSimilar structuralComparison (Web)
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    Biological Activity
    Description: Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol); it is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM. Imperatorin is a potent myorelaxant agent and acts as a calcium antagonist on vascular smooth muscle. Imperatorin has anticonvulsant, anti-inflammatory, anti-oxidant, neuroprotection, and anti-cancer effects, it also has been used in herbal formulations for the treatment of hypertension and cardiovascular diseases. Imperatorin dampens neuronal excitability by inhibiting voltage-gated Na + channels (VGSC), and blocks the HSP27 and HSP72 gene expression.
    Targets: COX | Caspase | HSP (e.g. HSP90) | Sodium Channel | Potassium Channel | Bcl-2/Bax | PPAR | NOS | BChE | TRPV1
    In vitro:
    Biomol Ther (Seoul). 2015 Sep; 23(5): 421–427.
    Imperatorin Suppresses Degranulation and Eicosanoid Generation in Activated Bone Marrow-Derived Mast Cells.[Pubmed: 26336581]
    Imperatorin has been known to exert many biological functions including anti-inflammatory activity.
    METHODS AND RESULTS:
    In this study, we investigated the inhibitory effects of Imperatorin on the production of inflammatory mediators in mouse bone marrow-derived mast cells (BMMC). Imperatorin inhibited degranulation and the generation of eicosanoids (leukotriene C4 (LTC4) and prostaglandin D2 (PGD2)) in IgE/antigen (Ag)-stimulated BMMC. To elucidate the molecular mechanism involved in this process, we investigated the effect of Imperatorin on intracellular signaling in BMMC. Biochemical analyses of the IgE/Ag-mediated signaling pathway demonstrated that Imperatorin dramatically attenuated degranulation and the production of 5-lipoxygenase-dependent LTC4 and cyclooxygenase-2-dependent PGD2 through the inhibition of intracellular calcium influx/phospholipase Cγ1, cytosolic phospholipase A2/mitogen-activated protein kinases and/or nuclear factor-κB pathways in BMMC.
    CONCLUSIONS:
    These results suggest that the effects of Imperatorin on inhibition of degranulation and eicosanoid generation through the suppression of multiple steps of IgE/Ag-mediated signaling pathways would be beneficial for the prevention of allergic inflammation.
    Oncol Rep. 2016 Apr;35(4):1995-2002.
    Imperatorin exhibits anticancer activities in human colon cancer cells via the caspase cascade.[Pubmed: 26794238 ]
    Despite advances in medical treatments for colon cancer, it remains one of the leading causes of cancer-related mortality among men. Thus, more efficacious treatment strategies for colon cancer are needed. Imperatorin is one of the major ingredients present in the root of Angelica dahurica, and has been used in herbal formulations for the treatment of hypertension and cardiovascular diseases. However, the medical properties of Imperatorin remain unclear.
    METHODS AND RESULTS:
    In the present study, the anti‑proliferative activities of Imperatorin were investigated in the HT‑29 colon cancer cell line. The results showed that Imperatorin significantly inhibited HT‑29 colon cancer cell growth with an IC50 value of 78 μM. Imperatorin induced the apoptosis of colon cancer cells through upregulation of p53 and the caspase cascade. Our findings revealed that Imperatorin induced cell cycle arrest in the G1 phase. The apoptotic index showed a steady increment when the Imperatorin concentration was increased.
    CONCLUSIONS:
    The results suggest that Imperatorin exerts considerable anti‑proliferative activities in HT‑29 colon cancer cells and highlight the potential of Imperatorin as an anticancer agent for colon cancer.
    Imperatorin Description
    Source: The roots of Angelica dahurica Benth. et Hook.
    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 3.6996 mL 18.498 mL 36.9959 mL 73.9919 mL 92.4898 mL
    5 mM 0.7399 mL 3.6996 mL 7.3992 mL 14.7984 mL 18.498 mL
    10 mM 0.37 mL 1.8498 mL 3.6996 mL 7.3992 mL 9.249 mL
    50 mM 0.074 mL 0.37 mL 0.7399 mL 1.4798 mL 1.8498 mL
    100 mM 0.037 mL 0.185 mL 0.37 mL 0.7399 mL 0.9249 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:
    Eur J Pharmacol. 2013 Dec 5;721(1-3):49-55.
    Suppression of voltage-gated Na(+) channels and neuronal excitability by imperatorin.[Pubmed: 24113522]
    Imperatorin is a naturally occurring furocoumarin compound isolated from plants such as Angelica archangelica and Cnidium monnieri. It has multiple pharmacological effects including anticonvulsant effects.
    METHODS AND RESULTS:
    Here we determined the effects of Imperatorin on voltage-gated Na(+) channels (VGSC) using whole-cell patch clamp techniques in differentiated neuronal NG108-15 cells. We showed that Imperatorin inhibited VGSC; such inhibition did not show state-dependence. Imperatorin caused a left shift in the steady-state inactivation curve without affecting activation gating. The inhibition of VGSC by Imperatorin displayed a mild frequency-dependence. Imperatorin was also shown to inhibit VGSC and action potential amplitude without affecting voltage-gated K(+) channels in rat hippocampal CA1 neurons.
    CONCLUSIONS:
    In conclusion, our results suggest that Imperatorin dampens neuronal excitability by inhibiting VGSC.
    Cell Research:
    Pharmacol Rep. 2014 Apr;66(2):292-300.
    The effect of quercetin and imperatorin on programmed cell death induction in T98G cells in vitro.[Pubmed: 24911084]
    High expression of HSP27 and HSP72 in glioma cells has been closely associated with chemoresistance and decreased sensitivity to programmed cell death induction. Therefore, it is important to devise therapies that effectively target invasive cancer cells by inducing cell death. The aim of our study was to assess the effect of quercetin and Imperatorin applied separately and in combinations on the apoptosis and autophagy induction in human T98G cells cultured in vitro.
    METHODS AND RESULTS:
    Cell death induction was analyzed by the staining method. The Western blotting technique and fluorimetric measurements of activity were used to assess the expression of marker proteins of apoptosis and autophagy. The specific siRNA transfected method was used for blocking of the expression of HSP27 and HSP72 genes. The experiments revealed the highest percentage of apoptotic cells after using a 50?M concentration of both compounds. Simultaneous quercetin and Imperatorin administration induced apoptosis more effectively than incubation with single drugs. These results were accompanied with decreased HSP27 and HSP72 expression, and a high level of caspase-3 and caspase-9 activity. Autophagy was not observed. Additional experiments were performed on a cell line with blocked Hsp27 and Hsp72 expression and significant increase the sensitivity to apoptosis induction upon quercetin and Imperatorin treatment was noticed.
    CONCLUSIONS:
    The present study indicates that quercetin and Imperatorin are potent apoptosis inducers, especially when they act synergistically, which may be a promising combination useful in glioma therapy. Our results also demonstrated that blocking the HSP27 and HSP72 gene expression might serve as a therapeutic target for the human brain cancer.
    Pharmacol Toxicol. 2002 Jul;91(1):40-8.
    Imperatorin, a furanocoumarin from Angelica dahurica (Umbelliferae), induces cytochrome c-dependent apoptosis in human promyelocytic leukaemia, HL-60 Cells.[Pubmed: 12193260]
    Imperatorin, a biologically active furanocoumarin from the roots of Angelica dahurica (Umbelliferae), was found to induce apoptosis in human promyelocytic leukaemia, HL-60 cells.
    METHODS AND RESULTS:
    DNA fragmentation assay, morphology-based evaluation, and flow cytometric analysis demonstrated that Imperatorin at micromolar concentrations was able to trigger apoptosis of HL-60 cells. Neither necrosis nor differentiation was observed at cytotoxic micromolar concentrations of Imperatorin. Further studies showed that the cytochrome c/caspase-9 pathway was responsible for Imperatorin-induced apoptosis; i.e., mitochondrial membrane was depolarized, Bcl-2 was down-regulated, cytochrome c was released from mitochondria, caspase-9 and caspase-3 were activated, and poly(ADP-ribose) polymerase was cleaved. Furthermore, Imperatorin-induced apoptosis was significantly blocked by Z-VAD-FMK (a broad spectrum caspase inhibitor), Z-LEHD-FMK (a caspase-9 inhibitor) and Ac-DMQD-CHO (a caspase-3 inhibitor), but not by Z-IEDT-FMK (a caspase-8 inhibitor).