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  • 海罂粟碱


    产品编号 CFN90408
    CAS编号 475-81-0
    分子式 = 分子量 C21H25NO4 = 355.43
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源 The tubers of Corydalis yanhusuo
    产品名称 产品编号 CAS编号 包装 QQ客服
    海罂粟碱 CFN90408 475-81-0 10mg QQ客服:1457312923
    海罂粟碱 CFN90408 475-81-0 20mg QQ客服:1457312923
    海罂粟碱 CFN90408 475-81-0 50mg QQ客服:1457312923
    海罂粟碱 CFN90408 475-81-0 100mg QQ客服:1457312923
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    Cell. 2018 Jan 11;172(1-2):249-261.e12.
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    doi: 10.1016/j.molcel.2017.10.022.

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
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    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.

    PMID: 28005066

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

    PMID: 30417089
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  • ...
  • 生物活性
    Description: Glaucine has antitussive, antioxidative potential and antiviral activities, it may be an anti-arthritic agent, it can enhance LPS and zymosan-induced IL-10 production. Glaucine can inhibit the migration and invasion of human breast cancer cells by MMP-9 inhibitory activity, attenuating IκBα and NF-κB activities.
    Targets: MMP(e.g.TIMP) | NF-kB | JAK | STAT | TLR | IL Receptor | TNF-α
    In vitro:
    Biochem Pharmacol. 2013 Nov 15;86(10):1497-506.
    Studies on the in vivo contribution of human cytochrome P450s to the hepatic metabolism of glaucine, a new drug of abuse.[Pubmed: 23988488]
    Glaucine ((S)-5,6,6a,7-tetrahydro-1,2,9,10-tetramethoxy-6-methyl-4H-dibenzo [de,g]quinoline), main isoquinoline alkaloid of Glaucium flavum (Papaveraceae), is used as antitussive, but also as recreational drug of abuse. Glaucine was mainly metabolized by O- and N-demethylation to four isomers in rats. So far, only scarce pharmacokinetic data were available. Therefore, the aim of the presented study was to assess the involvement of the ten most important cytochrome P450 (P450) isoforms in the main metabolic steps and determination of their kinetic parameters using the metabolite formation approach.
    Reference standards of investigated metabolites were synthesized for quantification. In addition, the impact of isomeric standards was tested for calibration and the use of simple peak area ratios on the kinetic constants and resulting contribution of P450 isoforms on estimated hepatic clearance. Kinetic profiles of all metabolite formations followed classic Michaelis-Menten behavior. Km values were between 25 and 140μM, Vmax between 0.10 and 1.92pmol/min/pmol. Using the relative activity factor approach, the hepatic clearance was calculated to be 27 and 73% for 2-O-demethylation by CYP1A2 and CYP3A4, 82, 3, and 15% for 9-O-demethylation by CYP1A2, CYP2C19, and CYP2D6, and finally <1 and 99% for N-demethylation by CYP2D6 and CYP3A4.
    These data were confirmed by inhibition tests. The calibration mode for determination of the metabolite concentrations had no relevant impact on the estimation of in vivo hepatic clearance of glaucine. As glaucine was metabolized via three initial steps and different P450 isoforms were involved in the hepatic clearance of glaucine, a clinically relevant interaction with single inhibitors should not be expected.
    Bioorg Med Chem. 2008 Aug 1;16(15):7457-61.
    Cinnamoyl- and hydroxycinnamoyl amides of glaucine and their antioxidative and antiviral activities.[Pubmed: 18590964 ]
    The aporphine alkaloid glaucine has been converted into 3-aminomethylglaucine and its free amino group has been linked to cinnamic, ferulic, sinapic, o-, and p-coumaric acids.
    The antioxidative potential of the synthesized amides was studied against DPPH(*) test. All of the tested compounds demonstrated higher radical scavenging activity than glaucine and 3-aminomethylglaucine, and lower antioxidative effect than the free hydroxycinnamic acids. The newly synthesized compounds were tested in vitro for antiviral activity against viruses belonging to different taxonomic groups.
    In vivo:
    Immunopharmacol Immunotoxicol. 2015 Feb;37(1):56-62.
    Acetylated derivative of glaucine inhibits joint inflammation in collagenase-induced arthritis.[Pubmed: 25328086]
    Osteoarthritis (OA) has become by far the most common joint disorder. A number of studies using OA animal models have explored the effects of agents that can modulate bone metabolism. In the present study, we investigated the effect of acetylated derivative of plant alkaloid glaucine (ADG) on experimental OA in mice.
    Arthritis was induced by two intraarticular (i.a.) injections of collaganase. Histopathological changes were observed through hematoxylin and eosine (H&E), safranin O and toluidine blue staining. Differentiation of bone marrow (BM) cells was evaluated by tartarate-resistant acid phosphatase (TRAP) assay. The expression of phospho-Janus kinase 2 (pJAK2) and phospho signal transducer and activator of transcription3 (pSTAT3) expression in the joints was determined by immunohistochemistry. We established that ADG significantly decreased cell infiltration (2.32 ± 0.14 versus 1.62 ± 0.13), cartilage loss (2.42 ± 0.12 versus 1.12 ± 0.10) and bone erosion (1.76 ± 0.13 versus 1.04 ± 0.14) in arthritic mice. It appeared that the substance inhibited in a dose-dependent manner osteoclast differentiation in vitro. ADG suppressed the expression of pJAK2 in the joint and partially affected the expression of pSTAT3.
    Present results suggest that ADG is a suitable candidate for further development as an anti-arthritic agent.
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.8135 mL 14.0675 mL 28.1349 mL 56.2699 mL 70.3373 mL
    5 mM 0.5627 mL 2.8135 mL 5.627 mL 11.254 mL 14.0675 mL
    10 mM 0.2813 mL 1.4067 mL 2.8135 mL 5.627 mL 7.0337 mL
    50 mM 0.0563 mL 0.2813 mL 0.5627 mL 1.1254 mL 1.4067 mL
    100 mM 0.0281 mL 0.1407 mL 0.2813 mL 0.5627 mL 0.7034 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.
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    N-甲基钓樟卡品; N-Methyllindcarpine CFN99454 14028-97-8 C19H21NO4 = 327.4 5mg QQ客服:2159513211
    异紫堇定碱; (+)-Isocorynoline CFN90215 475-67-2 C20H23NO4 = 341.40 20mg QQ客服:1457312923
    紫菫定酚; Corydine CFN90527 476-69-7 C20H23NO4 = 341.40 5mg QQ客服:2159513211
    紫堇块茎碱; Corytuberine CFN90528 517-56-6 C19H21NO4 = 327.37 5mg QQ客服:1457312923
    N-甲基-O10-甲基莲叶桐文; Litseglutine B CFN98279 25368-01-8 C20H23NO4 = 341.4 5mg QQ客服:3257982914
    波尔定碱; Boldine CFN98718 476-70-0 C19H21NO4 = 327.4 20mg QQ客服:2159513211
    无根藤辛; Cassythicine CFN98998 5890-28-8 C19H19NO4 = 325.4 5mg QQ客服:2056216494
    海罂粟碱; Glaucine CFN90408 475-81-0 C21H25NO4 = 355.43 20mg QQ客服:1457312923
    波尔定碱 2-甲醚; Lauroscholtzine CFN98078 2169-44-0 C20H23NO4 = 341.4 5mg QQ客服:2056216494
    Nantenine; Nantenine CFN89514 2565-01-7 C20H21NO4 = 339.38 5mg QQ客服:2159513211





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