CAS: 465-22-5; Scillarenin

该化合物是植物物种Scilla maritima(通称海葱)的糖浆, 被归类为心液胶, 也就是说它有能力影响心脏功能. Scillarenin 展示了一个具有糖味的类固醇核特征的结构, 典型地有助于其生物活动. 这个化合物有其潜在的治疗作用, 特别是在治疗心脏状况方面, 因为它可以提高心肌萎缩和心脏节奏. 但是, 与其他心脏胶垫一样, 它有一个狭窄的治疗窗口, 在较高剂量下具有毒性. Scillarenin 的溶液性受其血清特性的影响, 影响其在生物系统中的吸收和分布. 它的药理学特征包括积极的蛋白效应和潜在副作用, 需要在临床环境中使用时进行仔细监测. 总体来说, 硅素是心脏药理学和天然产品化学研究中的一个重要化合物.

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    Helleborogenone 41059-91-0
    3-巯基丙酸乙酯 Proscillaridin A 466-06-8

    合成工艺路线路线简述

      📜3-巯基丙酸乙酯置于acetate Buffer体系中,用 乙醇 作为反应溶剂,化学反应 6.5H,以100%的收率获得产物海葱苷元
      参考文献:Studies On Cardiac Ingredients Of Plants. Xi. Synthesis Of New Bufotoxin Homologues Utilizing Scillarenin (The Genuine Aglycone Of Proscillaridin),And Their Biological Activities.
      标题:Studies On Cardiac Ingredients Of Plants. Xi. Synthesis Of New Bufotoxin Homologues Utilizing Scillarenin (The Genuine Aglycone Of Proscillaridin),And Their Biological Activities.
      摘要:我们通过真正的苷元 Scillarenin (2),从 Proscillaridin (1) 制备出了具有不同长度烷基链(包括比甾体核 C-3 上的亚伯酰基更长的烷基链)的新 Bufotoxin 同源物 (3),产量极高.在制备过程中,我们为 1 的高效酶促糖酵解创造了条件,从而定量反应生成了 2.通过测量对自发性高血压大鼠肠系膜动脉平滑肌的影响,对狗肾脏制备的 Na+,K+-腺苷三磷酸酶(atpase)的抑制作用以及对离体豚鼠乳头肌制备的正性肌力作用(pie),评估了所制备的布福毒素同系物(3)的药理活性.布福毒素同系物(3)除了具有较高的 Na+,K+-Atpase 抑制活性和 Pie 外,还具有与临床常用的乌巴因,地高辛和地高辛相当的血管肌肉轻微收缩和小幅松弛作用.这些布福毒素同源物(3)可作为心脏病药物使用,对血管收缩的影响极小.
      DOI:10.1248/cpb.42.2256

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      专利信息


      专利号:US-10925977-B2
      优先权日:2006-10-05
      标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
      发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
      权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
      摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

      专利号:US-3682895-A
      优先权日:1970-07-17
      标题 :Synthesis of 3-hydroxy-5-bufa-20,22-dienolide
      发明人:PETTIT GEORGE R; FESSIER DYRAL C; PAUIL KENNETH D
      权利人:GEORGE R PETTIT; DYRAL C FESSIER; KENNETH D PAUIL
      摘要:THERE IS PROVIDED A NOVEL METHOD OF SYNTHEESIZING 5ABUFADIENOLIDES, WHICH ARE USEFUL INTERMEDIATES IN THE TOTAL SYNTHESIS OF BUFALIN, A CARDIAC ACTIVE COMPOUND. EPIANDROSTERONE ACETATE IS CONVERTED INTO 3B - ACETOXYL-5APREGNANE-21-AL WHICH UNDERGOES CHAIN EXTENSION TO METHYL 3B-ACETOXYL-20-FORMYL-21-NOR-5A-CHOLANATE WHICH IS RING CLOSED TO FORM THE 3B - ACETOXY-5-A-BUF-20(21)-ENOLIDE WHICH IS DEHYDROGENATED TO THE CORRESPONDING BUFADIENOLIDE.

      专利号:US-5455157-A
      优先权日:1989-05-22
      标 题:Method for the non-radioactive measurement of the nucleic acid synthesis in eukaryotic cells
      发明人:HINZPETER MATTHIAS; ELTZ HERBERT VON DER
      权利人:BOEHRINGER MANNHEIM GMBH
      摘要:For the determination of the rate of nucleic acid synthesis in eukaryotic cells a nucleotide which is non-radioactively labelled or derivatized with a hapten is introduced into the cells with the addition of liposomes and the rate of synthesis of the nucleic acids is determined by means of the incorporation of the nucleotide via its label or derivatization.

      专利号:WO-0112817-A1
      优先权日:1999-08-12
      标题:Evolution and use of enzymes for combinathorial and medicinal chemistry
      发明人:KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
      权利人:MAXYGEN INC; LIU LU; KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
      摘要:This invention provides libraries of recombinant derivatizing enzymes that are useful for biocatalytic synthesis of derivatives oforganic molecules, including lead compounds for pharmaceutical use. The recombinant derivatizing enzymes catalyze reactions such as modification or replacement of functional groups on the organicmolecules, or addition of chemical moieties onto preexisting functional groups. The use of recombinant enzyme libraries enables one to obtain enzymes that catalyze the formation of organic molecule derivatives that could not otherwise be made using only naturally occurring enzymes.

      专利号:US-10814013-B2
      优先权日:2006-10-05
      标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

      专利号:AU-2007308022-A2
      优先权日:2006-10-05
      标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

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      主要参考文献


      1: Sato N, Muro T. Antiviral activity of scillarenin, a plant bufadienolide. Jpn J Microbiol. 1974 Nov;18(6):441-8. doi: 10.1111/j.1348-0421.1974.tb00832.x.
      753:116-34. German. doi: 10.1002/jlac.19717530111.
      753:106-15. German. doi: 10.1002/jlac.19717530110. 7(4):191-205. 54(3):227-32. doi: 10.1055/s-2006-962412. 318(9):837-42. German. doi: 10.1002/ardp.19853180913. 318(10):882-8. German. doi: 10.1002/ardp.19853181005. 94(24):8592-3. doi: 10.1021/ja00779a057. 39(17):2629-31. doi: 10.1021/jo00931a041.

      合成参考文献


      摘要:Journal of Pharmacology and Experimental Therapeutics., 111(365), 1954 []
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