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  • 狗牙花定碱

    Coronaridine

    狗牙花定碱
    产品编号 CFN92859
    CAS编号 467-77-6
    分子式 = 分子量 C21H26N2O2 = 338.4
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源 The herbs of Ervatamia divaricata
    ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用
    提供自定义包装
    产品名称 产品编号 CAS编号 包装 QQ客服
    狗牙花定碱 CFN92859 467-77-6 1mg QQ客服:2056216494
    狗牙花定碱 CFN92859 467-77-6 5mg QQ客服:2056216494
    狗牙花定碱 CFN92859 467-77-6 10mg QQ客服:2056216494
    狗牙花定碱 CFN92859 467-77-6 20mg QQ客服:2056216494
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    ChemFaces的产品在许多优秀和顶级科学期刊中被引用

    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
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  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Biol Pharm Bull.2018, 41(11):1645-1651
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  • Lab Chip.2018, 18(6):971-978
  • J Basic Clin Physiol Pharmacol.2016, 27(1):1-8
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  • Appl Biochem Biotechnol.2020, 190(2):732-744
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  • Acta Biochim Pol.2015, 62(2):253-8
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  • Int Immunopharmacol.2019, 71:22-31
  • Toxins (Basel).2021, 13(12):898.
  • Mol Med Rep.2014, 9(5):1653-9
  • Fitoterapia.2022, 157:105130.
  • Metab Eng.2022, 75:143-152.
  • Front Plant Sci.2021, 12:673337.
  • Food Sci Nutr.2023, 11(9):5532-5542.
  • Curr Eye Res.2018, 43(1):27-34
  • Phytother Res.2022, 10.1002:ptr.7592.
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  • Green Chemistry2021, ISSUE 2.
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  • ...
  • 生物活性
    Description: Coronaridine is an antitumor agent. Coronaridine congeners inhibit hα3β4 AChRs by blocking the ion channel's lumen and probably by additional negative allosteric mechanisms by interacting with a series of non-luminal sites.
    Targets: AChR
    In vitro:
    Int J Biochem Cell Biol. 2015 Aug;65:81-90.
    Coronaridine congeners inhibit human α3β4 nicotinic acetylcholine receptors by interacting with luminal and non-luminal sites.[Pubmed: 26022277]
    To characterize the interaction of coronaridine congeners with human (h) α3β4 nicotinic acetylcholine receptors (AChRs), structural and functional approaches were used.
    METHODS AND RESULTS:
    The Ca(2+) influx results established that coronaridine congeners noncompetitively inhibit hα3β4 AChRs with the following potency (IC50's in μM) sequence: (-)-ibogamine (0.62±0.23)∼(+)-catharanthine (0.68±0.10)>(-)-ibogaine (0.95±0.10)>(±)-18-methoxycoronaridine [(±)-18-MC] (1.47±0.21)>(-)-voacangine (2.28±0.33)>(±)-18-methylaminocoronaridine (2.62±0.57 μM)∼(±)-18-hydroxycoronaridine (2.81±0.54)>(-)-noribogaine (6.82±0.78). A good linear correlation (r(2)=0.771) between the calculated IC50 values and their polar surface area was found, suggesting that this is an important structural feature for its activity. The radioligand competition results indicate that (±)-18-MC and (-)-ibogaine partially inhibit [(3)H]imipramine binding by an allosteric mechanism. Molecular docking, molecular dynamics, and in silico mutation results suggest that protonated (-)-18-MC binds to luminal [i.e., β4-Phe255 (phenylalanine/valine ring; position 13'), and α3-Leu250 and β4-Leu251 (leucine ring; position 9')], non-luminal, and intersubunit sites. The pharmacophore model suggests that nitrogens from the ibogamine core as well as methylamino, hydroxyl, and methoxyl moieties at position 18 form hydrogen bonds.
    CONCLUSIONS:
    Collectively our data indicate that coronaridine congeners inhibit hα3β4 AChRs by blocking the ion channel's lumen and probably by additional negative allosteric mechanisms by interacting with a series of non-luminal sites.
    Genet Mol Biol. 2013 Mar;36(1):105-10.
    Cytotoxicity and genotoxicity of coronaridine from Tabernaemontana catharinensis A.DC in a human laryngeal epithelial carcinoma cell line (Hep-2).[Pubmed: 23569415]
    Such as heyneanine, Coronaridine and voacangine.
    METHODS AND RESULTS:
    The aim of present study was firstly to screen the cytotoxic activity of the indole alkaloids heyneanine, Coronaridine and voacangine against HeLa (human cervix tumor), 3T3 (normal mouse embryo fibroblasts), Hep-2 (human laryngeal epithelial carcinoma) and B-16 (murine skin) cell lines by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide); and secondly to analyze the apoptotic activity, cell membrane damage and genotoxicity of the compound that showed the best cytotoxic activity against the tumor cell lines tested. Coronaridine was the one that exhibited greater cytotoxic activity in the laryngeal carcinoma cell line Hep-2 (IC50 = 54.47 μg/mL) than the other alkaloids tested (voacangine IC50 = 159.33 g/mL, and heyneanine IC50 = 689.45 μg/mL). Coronaridine induced apoptosis in cell lines 3T3 and Hep-2, even at high concentrations. The evaluation of genotoxicity by comet assay showed further that Coronaridine caused minimal DNA damage in the Hep-2 tumor cell line, and the LDH test showed that it did not affect the plasma membrane.
    CONCLUSIONS:
    These results suggest that further investigation of Coronaridine as an antitumor agent has merit.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.9551 mL 14.7754 mL 29.5508 mL 59.1017 mL 73.8771 mL
    5 mM 0.591 mL 2.9551 mL 5.9102 mL 11.8203 mL 14.7754 mL
    10 mM 0.2955 mL 1.4775 mL 2.9551 mL 5.9102 mL 7.3877 mL
    50 mM 0.0591 mL 0.2955 mL 0.591 mL 1.182 mL 1.4775 mL
    100 mM 0.0296 mL 0.1478 mL 0.2955 mL 0.591 mL 0.7388 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.
    部分图片展示
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    伏康京碱; Voacangine CFN92252 510-22-5 C22H28N2O3 = 368.5 5mg QQ客服:2056216494
    榴花碱; Conopharyngine CFN96068 76-98-2 C23H30N2O4 = 398.5 5mg QQ客服:3257982914
    20-羟基榴花碱; 19(S)-Hydroxyconopharyngine CFN96069 16790-93-5 C23H30N2O5 = 414.5 5mg QQ客服:2159513211
    Crassanine; Crassanine CFN96176 16790-92-4 C23H30N2O5 = 414.5 5mg QQ客服:1457312923
    长春质碱; Catharanthine CFN99765 2468-21-5 C21H24N2O2 = 336.43 20mg QQ客服:2159513211
    酒石酸长春质碱; Catharanthine Tartrate CFN90318 2648-21-5 C21H24N2O2.C4H6O6 = 486.40 20mg QQ客服:2056216494
    硫酸长春质碱; Catharanthine Sulfate CFN93298 70674-90-7 C21H26N2O6S = 434.51 5mg QQ客服:3257982914
    19,20-(E)-瓦来萨明碱; 19,20-(E)-Vallesamine CFN98432 3368-87-4 C20H24N2O3 = 340.4 5mg QQ客服:3257982914
    瓦来萨明碱 N-氧化物; Vallesamine N-oxide CFN99377 126594-73-8 C20H24N2O4 = 356.4 5mg QQ客服:2056216494
    去甲氧羰基蕊木碱甲酯; Methyl demethoxycarbonylchanofruticosinate CFN97275 80151-89-9 C21H24N2O3 = 352.4 5mg QQ客服:2056216494

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