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    Aconitine
    Information
    CAS No. 302-27-2 Price $80 / 20mg
    Catalog No.CFN99915Purity>=98%
    Molecular Weight645.75Type of CompoundAlkaloids
    FormulaC34H47NO11Physical DescriptionPowder
    Download Manual    COA    MSDSSimilar structuralComparison (Web)
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    Biological Activity
    Description: Aconitine, one of the major Aconitum alkaloids, is a highly toxic compound from the Aconitum species, it appears to exert a long-lasting cholinergic action in the causation of severe arrhythmias leading to death.
    Targets: P450 (e.g. CYP17)
    In vivo:
    Forensic Sci Int. 2005 Feb 10;148(1):21-9.
    Effects of long-term administrations of aconitine on electrocardiogram and tissue concentrations of aconitine and its metabolites in mice.[Pubmed: 15607586 ]
    Aconitum alkaloids are well known for their acute and high toxicity, for example, in the causation of severe arrhythmias leading to death. Aconitine, one of the major Aconitum alkaloids, is a highly toxic compound from the Aconitum species. However, there has been no studies reported on the influence of the chronic administration of Aconitine. Thus, this study was conducted to investigate the influence of chronic administration of Aconitine in experimental animal models.
    METHODS AND RESULTS:
    A dose of 1mg/kg per day was administered to the experimental animal models. We determined the concentration of Aconitine and its metabolites (benzoylaconine and aconine) in organs and blood with gas chromatography/selected ion monitoring (GC/SIM). In addition, we concurrently recorded the electrocardiogram (ECG). Fifteen minutes after administration on day 0, the early Aconitine administered group (acute group) revealed peak organ and blood concentration levels of Aconitine with a gradual decrease, thereafter. The concentration of Aconitine in organs and blood (from days 0 to 22; 90 min after the last administration of Aconitine) gradually decreased according to repeated administration, whereas benzoylaconine and aconine increased. ECG revealed various types of arrhythmias. However, the frequency of arrhythmias remarkably decreased with time and repeated administration of Aconitine.
    CONCLUSIONS:
    These results indicate two possibilities. First, the increase in the activity of Aconitine metabolism. Secondly, the decrease of effectiveness to the heart due to long-term (chronic) administration of Aconitine.
    Aconitine Description
    Source: The roots of Aconitum kusnezoffii Reichb.
    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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    Recently, ChemFaces products have been cited in many studies from excellent and top scientific journals

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
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    doi: 10.1016/j.molcel.2017.10.022.

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    Calculate Dilution Ratios(Only for Reference)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 1.5486 mL 7.7429 mL 15.4859 mL 30.9717 mL 38.7147 mL
    5 mM 0.3097 mL 1.5486 mL 3.0972 mL 6.1943 mL 7.7429 mL
    10 mM 0.1549 mL 0.7743 mL 1.5486 mL 3.0972 mL 3.8715 mL
    50 mM 0.031 mL 0.1549 mL 0.3097 mL 0.6194 mL 0.7743 mL
    100 mM 0.0155 mL 0.0774 mL 0.1549 mL 0.3097 mL 0.3871 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:
    Drug Metab Lett. 2014;8(2):135-44.
    The influences of aconitine, an active/toxic alkaloid from aconitum, on the oral pharmacokinetics of CYP3A probe drug buspirone in rats.[Pubmed: 25434398]
    Aconitine (AC), an active/toxic alkaloid from Aconitum species, is commonly present in Traditional Chinese Medicine (TCM) prescriptions because of the great effectiveness of Aconitum for the treatment of rheumatoid arthritis, cardiovascular diseases, and tumors in clinic. Buspirone (BP) is a sensitive CYP3A probe drug that is administered through oral/intravenous routes as recommended by the U.S. Food and Drug Administration.
    METHODS AND RESULTS:
    This study aims to investigate the influences of AC (0.125 mg/kg, oral) on first-pass (intestinal and hepatic) CYP3A activity by using oral BP as the probe in rats. The pharmacokinetics of oral buspirone hydrochloride at different doses (12.5, 25, and 50 mg/kg) were conducted. The pharmacokinetics of oral BP in rats pretreated with single dose or multiple doses (7-day) of AC were investigated. The plasma concentrations of BP and its major metabolites [1-(2-pyrimidinyl)piperazine (1-PP) and 6'-hydroxybuspirone (6'-OH-BP)] were determined. The formation ratios of 1-PP and 6'-OH-BP from BP (AUC0-∞ of 1-PP/AUC0-∞ of BP and AUC0-∞ of 6'-OH-BP/AUC0-∞ of BP values) showed no alternation when the dose of BP changed. Single dose of AC decreased the AUC0-∞ of BP by 53% but increased the formation ratio of 6'-OH-BP by 74% (P<0.05). Multiple AC exposure increased the AUC0-∞ of BP by 110%, and the formation ratios of 1-PP and 6'-OH-BP from BP were increased by 229% and decreased by 95%, respectively (P<0.05).
    CONCLUSIONS:
    Conclusively, single/multiple AC exposure did not alter the first-pass CYP3A activity when using oral BP as probe in rats. Nevertheless, multiple AC exposure had markedly changed the production of BP metabolites.
    Animal Research:
    J Cardiovasc Pharmacol. 1981 Jan-Feb;3(1):87-100.
    Hemodynamic and arrhythmogenic effects of aconitine applied to the left atria of anesthetized cats. Effects of amiodarone and atropine.[Pubmed: 6160357]

    METHODS AND RESULTS:
    The arrhythmogenic and hemodynamic effects of 0.04% Aconitine solution applied locally to the left atria of cats and the effects of amiodarone (10 mg/kg) and atropine (0.2 mg/kg) on the responses to Aconitine were investigated. Cats were anesthetized with sodium pentobarbital. The left atrial and limb lead electrocardiograms and the arterial pressure were recorded. Cardiac output was determined with the thermo dilution technique. Aconitine nitrate induced dysrhythmias lasting for a mean of 111 min. Atrial fibrillation occurred in 47% of the animals. A long-lasting (at least 3 hr) cardiodepressant action was seen in response to Aconitine. Pretreatment with atropine largely prevented the hemodynamic effects of Aconitine and prevented fibrillation. However, mean maximum atrial rates recorded during successive 5 min intervals were similar in control and atropine-treated animals. Amiodarone suppressed dysrhythmias in both atropine-treated and nontreated animals at a dose which exerted only minimal cardiodepression.
    CONCLUSIONS:
    The method described for evaluating potential activity against supraventricular dysrhythmias in the cat is relatively simple, reproducible, and suitable for statistical analyses. Aconitine appears to exert a long-lasting cholinergic action which may be involved in the genesis of Aconitine-induced atrial fibrillation.
    Structure Identification:
    J Pharm Sci. 2014 Nov;103(11):3602-10.
    An in vitro and in vivo comparison of solid and liquid-oil cores in transdermal aconitine nanocarriers.[Pubmed: 25187419]

    METHODS AND RESULTS:
    This study compared transdermal Aconitine delivery using solid lipid nanoparticles (SLN) and microemulsion (ME) vehicles. Aconitine-loaded SLN and ME were formulated with the same surfactant, cosurfactant, and water content, with an equal amount of oil matrix (ATO 888 for SLN and ethyl oleate for ME). These nanosized formulations (70-90 nm) showed suitable pH values and satisfactory skin tissue biocompatibility. SLN contained a higher concentration of smaller nanoparticles, compared with that in ME. Neither of the nanocarriers penetrated across excised skin in their intact form. In vitro transdermal delivery studies found that transdermal Aconitine flux was lower from SLN than from ME (p < 0.05), but skin Aconitine deposition was higher using SLN (p < 0.05). Fluorescence-activated cell sorting indicated that in vitro uptake of fluorescently labeled SLN by human immortalized keratinocyte (HaCaT) cells was greater than that of ME, indicating that a transcellular pathway may contribute to cutaneous drug absorption more effectively from SLN.
    CONCLUSIONS:
    In vivo studies found that these formulations could loosen stratum corneum layers and increase skin surface crannies, which may also enhance transdermal Aconitine delivery. SLN produced a more sustained Aconitine release, indicating that compared with ME, this transdermal delivery vehicle may reduce the toxicity of this drug.
    Zhong Yao Cai. 2014 Feb;37(2):284-7.
    [Pharmacokinetic study of six aconitine alkaloids in aconiti lateralis radix praeparata in beagle dogs].[Pubmed: 25095352]
    To study the pharmacokinetics characteristics of six Aconitum alkaloids Aconitine (AC), mesAconitine (MA), hypAconitine (HA), benzoylaconine (BAC), benzoylmesaconine (BMA) and benzoylhypaconine (BHA) in beagle dogs.
    METHODS AND RESULTS:
    An ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed for simultaneous quantitation of six Aconitum alkaloids in beagle dog plasma after oral administration of Aconiti Lateralis Radix Praeparata decoction. UPLC/MS/MS system coupled with an electrospray ionization (ESI) source was performed in multiple-reaction monitoring (MRM) mode. Sample preparation was performed with solid-phase extraction(SPE) on a 3 mL HLB cartridge before the analysis. The separation was applied on a Waters C8 column (100 mm x 2.1 mm, 1.7 microm) and a gradient elution of methanol and 0.2% formic acid-water was used as mobile phase. The pharmacokinetic parameters were calculated by the results of the analysis through the DAS 2. 1 software (Drug and Statistics for Windows). The results showed that the fitting model for the six Aconitum alkaloids was the one-compartment model pharmacokinetics.
    CONCLUSIONS:
    The method is successfully used for the pharmacokinetic evaluation of the six Aconitum alkaloids in beagle dog plasma, it can help monitor the ADME/Tox process when taking Aconiti Lateralis Radix Praeparata by observing the pharmacokinetic process. The results provide a good reference for clinical treatment and safe application of Aconiti Lateralis Radix Praeparata.