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    Paeonol
    Information
    CAS No. 552-41-0 Price $30 / 20mg
    Catalog No.CFN98926Purity>=98%
    Molecular Weight166.2 Type of CompoundPhenols
    FormulaC9H10O3Physical DescriptionPowder
    Download Manual    COA    MSDSSimilar structuralComparison (Web)
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    Biological Activity
    Description: Paeonol has anticancer, anti-inflammatory, antioxidant and cardiovascular protective activities, it shows a novel inhibitory role on neuroinflammation, and presents a new candidate agent for the development of therapies for inflammation-related neurodegenerative diseases. Paeonol suppresses lipopolysaccharide-induced inflammatory cytokines in macrophage cells and protects mice from lethal endotoxin shock. Paeonol inhibits MAO-A and MAO-B with IC50 of 54.6 μM and 42.5 μM, respectively; it inhibits PGE₂ synthesis and COX-2 expression, and modulates Sirtuin 1, PKCδ and c-Src signaling pathway.
    Targets: NO | NOS | AMPK | TNF-α | PKC | PGE | COX | ROS | GSK-3 | p53 | IL Receptor | p38MAPK | JNK | ERK | IkB | Caspase | Bcl-2/Bax | p65 | NF-kB | IKK | MAO-A | MAO-B | Src
    In vitro:
    J Ethnopharmacol. 2014 Jun 11;154(2):428-36.
    Paeonol protects against premature senescence in endothelial cells by modulating Sirtuin 1 pathway.[Pubmed: 24768807]
    Paeonol is a phenolic compound isolated mainly from Moutan cortex, root bark of Chinese Peony tree. Moutan cortex holds a significant value in traditional Chinese medicine for alleviating various oxidative stress-related diseases mainly atherosclerosis and myocardial infarction. The present study seeks to identify the protective mechanisms of Paeonol in oxidative stress-induced premature senescence in endothelial cells.
    METHODS AND RESULTS:
    HUVECs were pretreated with Paeonol or DMSO control at different doses for 24h prior to an exposure of 200μM of reactive oxygen species (ROS) inducer, hydrogen peroxide (H2O2). The protective effects of Paeonol against H2O2-induced senescence were evaluated and the activation of Sirtuin 1 pathway by Paeonol pretreatment was investigated in HUVECs. Paeonol attenuated H2O2-induced cell growth arrest at G0/G1 phase, reduced the percentage of SA-β-Gal positive cells and increased BrdU incorporation. In addition, enzymatic Sirt1 activation assay indicated that Paeonol significantly increased lysyl deactylase activity of Sirt1 enzyme with a fold change of 2.4±0.195 (p<0.05). Furthermore, pretreatment with Paeonol significantly decreased the levels of p53, acetyl H3K14 and H4K16 protein expression upregulated by H2O2 stimulation. The changes in the histone protein levels were accompanied with an increase in Sirt1 protein expression level.
    CONCLUSIONS:
    These findings suggest that Paeonol protects endothelial cells against oxidative stress-induced premature senescence by modulating the expressions of Sirt1 protein and its substrates.
    Int J Mol Sci. 2014 Jul 2;15(7):11760-72.
    Paeonol suppresses chondrosarcoma metastasis through up-regulation of miR-141 by modulating PKCδ and c-Src signaling pathway.[Pubmed: 24992595]
    Chondrosarcoma, a primary malignant bone cancer, has potential for local invasion and distant metastasis, especially to the lungs. Patients diagnosed with it show poor prognosis. Paeonol (2'-hydroxy-4'-methoxyacetophenone), the main active compound of traditional Chinese remedy Paeonia lactiflora Pallas, exhibits anti-inflammatory and anti-tumor activity; whether Paeonol regulates metastatic chondrosarcoma is largely unknown.
    METHODS AND RESULTS:
    Here, we find Paeonol do not increase apoptosis. By contrast, at non-cytotoxic concentrations, Paeonol suppresses migration and invasion of chondrosarcoma cells. We also demonstrate Paeonol enhancing miR-141 expression and miR-141 inhibitor reversing Paeonol-inhibited cell motility; Paeonol also reduces protein kinase C (PKC)d and c-Src kinase activity.
    CONCLUSIONS:
    Since Paeonol inhibits migration and invasion of human chondrosarcoma via up-regulation of miR-141 via PKCd and c-Src pathways, it thus might be a novel anti-metastasis agent for treatment of metastatic chondrosarcoma.
    Int Immunopharmacol. 2007 Mar;7(3):343-50.
    Paeonol suppresses intercellular adhesion molecule-1 expression in tumor necrosis factor-alpha-stimulated human umbilical vein endothelial cells by blocking p38, ERK and nuclear factor-kappaB signaling pathways.[Pubmed: 17276892 ]
    Paeonol (2'-hydroxy-4'-methoxyacetophenone), the main active compound of the traditionally used Chinese herb Paeonia lactiflora Pallas, has anti-inflammatory, antioxidant and cardiovascular protective activities.
    METHODS AND RESULTS:
    We studied how the levels of intercellular adhesion molecule-1 (ICAM-1), one of the key molecules in the development of atherosclerosis, might be affected by Paeonol in tumor necrosis factor-alpha (TNF-alpha)-activated human umbilical vein endothelial cells (HUVECs). Paeonol concentration-dependently inhibited the production of ICAM-1; it inhibited nuclear factor-kappaB (NF-kappaB) p65 translocation into the nucleus and the phosphorylation of inhibitory factor kappaBalpha (IkappaBalpha). It also blocked the TNF-alpha-induced phosphorylation of p38 and extracellular signal-regulated kinase (ERK), which are involved in regulating ICAM-1 production by TNF-alpha. Paeonol inhibited U937 monocyte adhesion to HUVECs stimulated by TNF-alpha, suggesting that it may inhibit the binding of monocytes to endothelium by regulating the production of critical adhesion molecules by TNF-alpha. The inhibitory effect of Paeonol on ICAM-1 production might be mediated by inhibiting p38, ERK and NF-kappaB signaling pathways, which are involved in TNF-alpha-induced ICAM-1 production.
    CONCLUSIONS:
    Thus, Paeonol may be beneficial in the treatment of cardiovascular disorders such as atherosclerosis.
    In vivo:
    Int J Mol Sci. 2015 Apr 21;16(4):8844-60.
    Effects of paeonol on anti-neuroinflammatory responses in microglial cells.[Pubmed: 25906473]
    Increasing studies suggest that inflammatory processes in the central nervous system mediated by microglial activation plays an important role in numerous neurodegenerative diseases. Development of planning for microglial suppression is considered a key strategy in the search for neuroprotection. Paeonol is a major phenolic component of Moutan Cortex, widely used as a nutrient supplement in Chinese medicine. In this study, we investigated the effects of Paeonol on microglial cells stimulated by inflammagens.
    METHODS AND RESULTS:
    Paeonol significantly inhibited the release of nitric oxide (NO) and the expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Treatment with Paeonol also reduced reactive oxygen species (ROS) production and inhibited an ATP-induced increased cell migratory activity. Furthermore, the inhibitory effects of neuroinflammation by Paeonol were found to be regulated by phosphorylated adenosine monophosphate-activated protein kinase-α (AMPK-α) and glycogen synthase kinase 3 α/β (GSK 3α/β). Treatment with AMPK or GSK3 inhibitors reverse the inhibitory effect of neuroinflammation by Paeonol in microglial cells. Furthermore, Paeonol treatment also showed significant improvement in the rotarod performance and microglial activation in the mouse model as well.
    CONCLUSIONS:
    The present study is the first to report a novel inhibitory role of Paeonol on neuroinflammation, and presents a new candidate agent for the development of therapies for inflammation-related neurodegenerative diseases.
    Paeonol Description
    Source: The roots of Paeonia moutan Sim.
    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 6.0168 mL 30.0842 mL 60.1685 mL 120.3369 mL 150.4212 mL
    5 mM 1.2034 mL 6.0168 mL 12.0337 mL 24.0674 mL 30.0842 mL
    10 mM 0.6017 mL 3.0084 mL 6.0168 mL 12.0337 mL 15.0421 mL
    50 mM 0.1203 mL 0.6017 mL 1.2034 mL 2.4067 mL 3.0084 mL
    100 mM 0.0602 mL 0.3008 mL 0.6017 mL 1.2034 mL 1.5042 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
    Cell Research:
    Oncol Rep. 2014 Dec;32(6):2845-53.
    Paeonol exerts an anticancer effect on human colorectal cancer cells through inhibition of PGE₂ synthesis and COX-2 expression.[Pubmed: 25322760]
    Cyclooxygenase-2 (COX-2) and its metabolite prostaglandin E2 (PGE2) can potentially affect most of the events in cancer development, including promotion of proliferation, resistance to apoptosis, angiogenesis, immune suppression and invasion. However, worldwide attention has predominantly centered on the cardiovascular toxicity of selective COX-2 inhibitors. Paeonol is a major active extract from the root bark of Paeonia suffruticosa Andrews with anti‑inflammatory, anti-oxidant, anti-allergic, anti-oxidation and antitumor effects. In the present study, we investigated the underlying mechanisms of Paeonol in inducing apoptosis and aimed to ascertain whether its antitumor effect is associated with a reduction in COX-2 expression and a decrease in the levels of PGE2 in colorectal cancer cells.
    METHODS AND RESULTS:
    We observed that Paeonol inhibited cell proliferation and induced apoptosis in a dose- and time-dependent manner in colorectal cancer cells, which was associated with a reduction in COX-2 expression and PGE2 synthesis. Treatment with the selective COX-2 inhibitor, celecoxib, or transient transfection of colorectal cancer cells with COX-2 siRNA, also inhibited cell proliferation and induced apoptosis. Western blot analysis showed that Paeonol inhibited the activation of NF-κB, an upstream regulator of COX-2, and its translocation to the nucleus. Treatment with increasing doses of Paeonol led to increased expression of pro-apoptotic factor Bax and decreased expression of anti-apoptotic factor Bcl-2. Caspase-3 and caspase-9 were activated, and Paeonol induced loss of mitochondrial membrane potential, suggesting that the apoptosis induced by Paeonol was mediated by mitochondrial pathways. In addition, Paeonol significantly suppressed tumor growth in a xenograft tumor mouse model in a dose-dependent manner.
    CONCLUSIONS:
    Our findings indicate that Paeonol exerts an antitumor effect on human colorectal cancer cells by inhibiting PGE2 production and COX-2 expression. We expect that Paeonol may replace selective COX-2 inhibitors due to their toxic effects, and may offer a new strategy for the therapy of colorectal cancer.
    Animal Research:
    Fundam Clin Pharmacol. 2014 Jun;28(3):268-76.
    Paeonol suppresses lipopolysaccharide-induced inflammatory cytokines in macrophage cells and protects mice from lethal endotoxin shock.[Pubmed: 23413967]
    Paeonol (2'-hydroxy-4'-methoxyacetophenone) is the main phenolic compound of the radix of Paeonia suffruticosa which has been used as traditional Chinese medicine. In this study, we primarily investigated the anti-inflammatory effects and the underlying mechanisms of Paeonol in RAW macrophage cells; and based on these effects, we assessed the protective effects of Paeonol on lipopolysaccharide-induced endotoxemia in mice.
    METHODS AND RESULTS:
    The in vitro study showed that Paeonol regulated the production of TNF-α, IL-1β, IL-6, and IL-10 via inactivation of IκBα, ERK1/2, JNK, and p38 MAPK. In mouse model of lipopolysaccharide-induced endotoxemia, pro- and anti-inflammatory cytokines are significantly regulated, and thus the survival rates of lipolysaccharide-challenged mice are improved by Paeonol (150, 200, or 250 mg/kg).
    CONCLUSIONS:
    Therefore, Paeonol has a beneficial activity against lipopolysaccharide-induced inflammation in RAW 264.7 cell and mouse models.