Info: Read More
  • ChemFaces is a professional high-purity natural products manufacturer.
  • Product Intended Use
  • 1. Reference standards
  • 2. Pharmacological research
  • 3. Inhibitors
  •   
  • Home
  • Natural Products
  • Bioactive
  • Screening Libraries
  • Hot Products
  • Plant Catalog
  • Customer Support
  • Product Use Citation
  • About Us
  • Contact Us
  • Science | Nature | Cell | View More
    Natural Products
    Axillaridine A
    Axillaridine A
    Information
    CAS No. 128255-16-3 Price
    Catalog No.CFN99386Purity>=98%
    Molecular Weight462.7 Type of CompoundAlkaloids
    FormulaC30H42N2O2Physical DescriptionPowder
    Download Manual    COA    MSDS    SDFSimilar structuralComparison (Web)  (SDF)
    Citing Use of our Products
    How to Order
    Orders via your E-mail:

    1. Product number / Name / CAS No.
    2. Delivery address
    3. Ordering/billing address
    4. Contact information
    Sent to Email: info@chemfaces.com
    Contact Us
    Order & Inquiry & Tech Support

    Tel: (0086)-27-84237683
    Fax: (0086)-27-84254680
    E-mail: manager@chemfaces.com
    Address: No. 83, CheCheng Rd., WETDZ, Wuhan, Hubei 430056, PRC
    Delivery time
    Delivery & Payment method

    1. Usually delivery time: Next day delivery by 9:00 a.m. Order now

    2. We accept: Wire transfer & Credit card & Paypal & Western Union
    * Packaging according to customer requirements(5mg, 10mg, 20mg and more). We shipped via FedEx, DHL, UPS, EMS and others courier.
    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
    Other Packaging *Packaging according to customer requirements(100uL/well, 200uL/well and more), and Container use Storage Tube With Screw Cap
    Our products had been exported to the following research institutions and universities, And still growing.
  • Stanford University (USA)
  • Universidad Miguel Hernández (Spain)
  • University of Otago (New Zealand)
  • Macau University of Science and... (China)
  • Kyushu University (Japan)
  • Kazusa DNA Research Institute (Japan)
  • Universite Libre de Bruxelles (Belgium)
  • Aarhus University (Denmark)
  • Universitas Airlangga (Indonesia)
  • University of Brasilia (Brazil)
  • Chang Gung University (Taiwan)
  • More...
  • Package
    Featured Products
    3,4-Di-O-caffeoylquinic acid methy...

    Catalog No: CFN90856
    CAS No: 114637-83-1
    Price: $388/5mg
    Platycodigenin

    Catalog No: CFN92207
    CAS No: 22327-82-8
    Price: $268/10mg
    Ginsenoside Rk2

    Catalog No: CFN92818
    CAS No: 364779-14-6
    Price: $318/5mg
    Angustifoline

    Catalog No: CFN92233
    CAS No: 550-43-6
    Price: $490/5mg
    Leachianone A

    Catalog No: CFN97560
    CAS No: 97938-31-3
    Price: $218/5mg
    Dihydrocucurbitacin B

    Catalog No: CFN92140
    CAS No: 13201-14-4
    Price: $318/10mg
    Ganoderol A

    Catalog No: CFN99065
    CAS No: 104700-97-2
    Price: $488/5mg
    Related Screening Libraries
    Size /Price /Stock 10 mM * 100 uL in DMSO / Inquiry / In-stock
    10 mM * 1 mL in DMSO / Inquiry / In-stock
    Related Libraries
  • Inhibitors Compound Library
  • Neuroprotection Compound Library
  • Alkaloids Compound Library
  • Biological Activity
    Description: Axillaridine A is a new cholinesterase inhibitors, it may act as potential leads in the discovery of clinically useful inhibitors for nervous-system disorders, particularly by reducing memory deficiency in Alzheimer’s disease patients by potentiating and effecting the cholinergic transmission process. (+)-Axillaridine A has significant activity as antiestrogen binding site (AEBS)-inhibitory agents.
    In vitro:
    J Nat Prod. 1998 Oct;61(10):1257-62.
    Activity-guided isolation of steroidal alkaloid antiestrogen-binding site inhibitors from Pachysandra procumbens.[Pubmed: 9784163]

    METHODS AND RESULTS:
    Four novel steroidal alkaloids, (+)-(20S)-20-(dimethylamino)-3-(3'alpha-isopropyl)-lactam-5alpha-+ ++preg n-2-en-4-one (1), (+)-(20S)-20-(dimethylamino)-16alpha-hydroxy-3-(3'alpha-isopropyl) -la ctam-5alpha-pregn-2-en-4-one (2), (+)-(20S)-3-(benzoylamino)-20-(dimethylamino)-5alpha-pregn-2-en-++ +4beta -yl acetate (3), and (+)-(20S)-2alpha-hydroxy-20-(dimethylamino)-3beta-phthalimido-5 alpha- pregnan-4beta-yl acetate (4), as well as five known compounds, (-)-pachyaximine A (5), (+)-spiropachysine (6), (+)-Axillaridine A (7), (+)-epipachysamine D (8), and (+)-pachysamine B (9), were isolated from Pachysandra procumbens, using a bioassay-guided fractionation based on inhibition of 3H-tamoxifen binding at the antiestrogen binding site (AEBS).
    CONCLUSIONS:
    Compounds 1-7 and 9 demonstrated significant activity as AEBS-inhibitory agents, and compounds 3, 5 and 9 were found to potentiate significantly the antiestrogenic effect mediated by tamoxifen in cultured Ishikawa cells. The structure elucidation of compounds 1-4 was carried out by spectral data interpretation.
    Axillaridine A Description
    Source: The herbs of Pachysandra axillaris
    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.
    Recent ChemFaces New Products and Compounds
    Lappaol B

    Catalog No: CFN95242
    CAS No: 62359-60-8
    Price: $333/10mg
    Isomucronulatol

    Catalog No: CFN90839
    CAS No: 52250-35-8
    Price: $218/10mg
    Isoliquiritin apioside

    Catalog No: CFN90800
    CAS No: 120926-46-7
    Price: $288/10mg
    Mulberroside F

    Catalog No: CFN90794
    CAS No: 193483-95-3
    Price: $288/10mg
    Licoisoflavone A

    Catalog No: CFN90816
    CAS No: 66056-19-7
    Price: $268/5mg
    Kakkalide

    Catalog No: CFN95052
    CAS No: 58274-56-9
    Price: $260/10mg
    2-Methoxyfuranoguaia-9-ene-8-one

    Catalog No: CFN95220
    CAS No: 88010-62-2
    Price: $318/10mg
    Hamaudol

    Catalog No: CFN95115
    CAS No: 735-46-6
    Price: $318/10mg
    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.
    doi: 10.1016/j.cell.2017.12.019.
    IF=36.216(2019)

    PMID: 29328914

    Cell Metab. 2020 Mar 3;31(3):534-548.e5.
    doi: 10.1016/j.cmet.2020.01.002.
    IF=22.415(2019)

    PMID: 32004475

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.
    IF=14.548(2019)

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
    doi: 10.1021/acsnano.7b08969.
    IF=13.903(2019)

    PMID: 29553709

    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.
    IF=13.297(2019)

    PMID: 28005066

    Sci Adv. 2018 Oct 24;4(10): eaat6994.
    doi: 10.1126/sciadv.aat6994.
    IF=12.804(2019)

    PMID: 30417089
    Calculate Dilution Ratios(Only for Reference)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.1612 mL 10.8061 mL 21.6123 mL 43.2246 mL 54.0307 mL
    5 mM 0.4322 mL 2.1612 mL 4.3225 mL 8.6449 mL 10.8061 mL
    10 mM 0.2161 mL 1.0806 mL 2.1612 mL 4.3225 mL 5.4031 mL
    50 mM 0.0432 mL 0.2161 mL 0.4322 mL 0.8645 mL 1.0806 mL
    100 mM 0.0216 mL 0.1081 mL 0.2161 mL 0.4322 mL 0.5403 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:
    Helv. Chim. Acta, 2002, 85(2):678-88.
    Pregnane-Type Steroidal Alkaloids of Sarcococca saligna: A New Class of Cholinesterase Inhibitors[Reference: WebLink]

    METHODS AND RESULTS:
    The structures of the new alkaloids salignenamide C (1), salignenamide D (2), 2b-hydroxyepipachysamine D (3), salignenamide E (4), and salignenamide F (5) were elucidated with the help of modern spectroscopic techniques, while the known alkaloids axillarine C (6), axillarine F (7), sarcorine (8), N 3 -demethylsaracodine (9), saligcinnamide (10), salignenamide A (11), vaganine A (12), Axillaridine A (13), sarsalignone (14), and sarsalignenone (15) were identified by comparing their spectral data with those reported earlier. Inhibition of electric-eel acetylcholinesterase (EC 3.1.1.7) and horse-serum butyrylcholinesterase (EC 3.1.1.8) by alkaloids 1 ± 15 were investigated.
    CONCLUSIONS:
    These new cholinesterase inhibitors may act as potential leads in the discovery of clinically useful inhibitors for nervous-system disorders, particularly by reducing memory deficiency in Alzheimer×s disease patients by potentiating and effecting the cholinergic transmission process.
    Structure Identification:
    J Enzyme Inhib Med Chem. 2009 Oct;24(5):1101-5.
    Molecular dynamics simulation of Axillaridine-A: a potent natural cholinesterase inhibitor.[Pubmed: 19555175]
    Molecular Dynamics (MD) simulations were carried out for human acetylcholinesterase (hAChE) and its complex with Axillaridine A, in order to dynamically explore the active site of the protein and the behaviour of the ligand at the peripheral binding site.
    METHODS AND RESULTS:
    Simulation of the enzyme alone showed that the active site of AChE is located at the bottom of a deep and narrow cavity whose surface is lined with rings of aromatic residues while Tyr72 is almost perpendicular to the Trp286, which is responsible for stable pi -pi interactions. The complexation of AChE with Axillaridine A, results in the reduction of gorge size due to interaction between the ligand and the active site residues. The gorge size was determined by the distance between the center of mass of Glu81 and Trp286. As far as the geometry of the active site is concerned, the presence of ligand in the active site alters its specific conformation, as revealed by stable hydrogen bondings established between amino acids. With the increasing interaction between ligand and the active amino acids, size of the active site of the complex decreases with respect to time.
    CONCLUSIONS:
    Axillaridine A, forms stable pi -pi interactions with the aromatic ring of Tyr124 that results in inhibition of catalytic activity of the enzyme. This pi -pi interaction keeps the substrate stable at the edge of the catalytic gorge by inhibiting its catalytic activity. The MD results clearly provide an explanation for the binding pattern of bulky steroidal alkaloids at the active site of AChE.