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    Natural Products
    Humantenirine
    Humantenirine
    Information
    CAS No. 82375-30-2 Price
    Catalog No.CFN97983Purity>=98%
    Molecular Weight370.5Type of CompoundAlkaloids
    FormulaC21H26N2O4Physical DescriptionPowder
    Download     COA    MSDSSimilar structuralComparison (Web)
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    According to end customer requirements, ChemFaces provide solvent format. This solvent format of product intended use: Signaling Inhibitors, Biological activities or Pharmacological activities.
    Size /Price /Stock 10 mM * 1 mL in DMSO / Inquiry
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    Related Screening Libraries
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    10 mM * 1 mL in DMSO / Inquiry / In-stock
    Related Libraries
  • Alkaloids Compound Library
  • P450 (e.g. CYP17) Inhibitor Library
  • Biological Activity
    Description: Standard reference
    Targets: P450 (e.g. CYP17)
    In vitro:
    J Nat Prod. 1987 Mar-Apr;50(2):195-8.
    Cytotoxic steroids of Gelsemium sempervirens.[Pubmed: 3655795]

    METHODS AND RESULTS:
    A new pregnane derivative, 12 beta-hydroxy-5 alpha-pregn-16-ene-3,20-dione, along with the known derivative 12 beta-hydroxy-pregna-4,16-diene-3,20-dione have been isolated from a MeOH extract of the stem of Gelsemium sempervirens and found to be the principal cytotoxic entities. The 13C-nmr spectra of both compounds were assigned by comparison with other pregnane analogs thereby allowing confirmation of the stereochemistry at C-5 in compound. Heteronuclear 2D correlation and selective INEPT experiments indicated the need to revise a number of 13C-nmr assignments of pregn-4,16-dien-3,20-dione.
    CONCLUSIONS:
    Nine indole alkaloids, gelsemine, gelsevirine, 21-oxogelsemine, gelsedine, 14 beta-hydroxygelsedine, gelsenicine, humantenidine, Humantenirine, and koumidine were found to be inactive in the KB and P-388 cytotoxicity test systems.
    Humantenirine Description
    Source: The herbs of Gelsemium sempervirens
    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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    IF=36.216(2019)

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    Calculate Dilution Ratios(Only for Reference)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.6991 mL 13.4953 mL 26.9906 mL 53.9811 mL 67.4764 mL
    5 mM 0.5398 mL 2.6991 mL 5.3981 mL 10.7962 mL 13.4953 mL
    10 mM 0.2699 mL 1.3495 mL 2.6991 mL 5.3981 mL 6.7476 mL
    50 mM 0.054 mL 0.2699 mL 0.5398 mL 1.0796 mL 1.3495 mL
    100 mM 0.027 mL 0.135 mL 0.2699 mL 0.5398 mL 0.6748 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:
    J Ethnopharmacol. 2015 May 26;166:66-73.
    Inhibitory effects of cytochrome P450 enzymes CYP1A2, CYP2A6, CYP2E1 and CYP3A4 by extracts and alkaloids of Gelsemium elegans roots.[Pubmed: 25764964 ]
    Gelsemium elegans (GE), widely distributed in East Asia, South East Asia and Northern America, is a kind of well-known toxic plant throughout the world. Yet it has been used as a Chinese folk medicine for treatment of malignant tumors, pain, rheumatic arthritis, psoriasis and immune function. The present study was to investigate the potential inhibitory effects of G. elegans (GE) roots on four major cytochrome P450 (CYP450) isoforms (CYP1A2, CYP2A6, CYP2E1 and CYP3A4) in vitro.
    METHODS AND RESULTS:
    Four extracts (petroleum ether, dichloromethane, EtOAc and aqueous) of GE and two commercially available alkaloids (koumine and humantenmine) were screened for their CYP isoforms inhibitory activity. Four enzyme inhibition assays were examined according to the method of the literature. Phenacetin, coumarin, chlorzoxazone and testosterone were used as probe substrates in order to determine CYP1A2, CYP2A6, CYP2E1 and CYP3A4 catalytic activity, respectively. Each probe substrate was incubated with or without each extract and active constituent for corresponding isoform, followed by determination of the kinetics parameters, IC50 and Ki, to characterize inhibitory effects. GE dichloromethane extract selectively inhibited activities of CYP2E1 (IC50=29.04µg/ml) and CYP2A6 (IC50=46.84µg/ml), with Ki of 10.16 and 19.33µg/ml, respectively. In the case of alkaloids, koumine exhibited significant inhibitory effects on CYP2E1 while humantenmine showed more potent inhibition on CYP2E1 and CYP2A6 (IC50 of 47.44, 18.34 and 45.87µg/ml, Ki of 31.20, 35.06 and 52.06µg/ml, respectively). Because of their relatively high Ki values, the active constituents in GE dichloromethane extract were analyzed. The UPLC-DAD-ESI-MS/MS data showed that GE dichloromethane extract contains 6 kinds of indole alkaloids (koumine, humantenmine, humantenine, Humantenirine, N-methoxytaberpsychine, and sempervirine). As for CYP1A2 and CYP3A4, the negligible inhibitions were observed.
    CONCLUSIONS:
    G. elegans extracts inhibited several CYP450 enzyme activities with varying potency. Strong inhibition was observed in CYP2E1 and CYP2A6 isoforms by GE dichloromethane extract, koumine and humantenmine, inferring the involvement of alkaloids chemical constituents from GE dichloromethane extract in the effect.