CAS: 466-06-8; 5-((3S,8R,9S,10R,13R,14S,17R)-14-Hydroxy-10,13-Dimethyl-3-(((2R,3R,4R,5R,6S)-3,4,5-Trihydroxy-6-Methyltetrahydro-2H-Pyran-2-yl)Oxy)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-Tetradecahydro-1H-Cyclopenta[a]Phenanthren-17-yl)-2H-Pyran-2-One

该化合物是植物物种Scilla maritima(通称海螺)的心脏胶片,该化合物展示了一种具有内酯环的类固醇核结构,典型的是一种心液球环,而这种环状体是心脏液晶体素.人们知道Proscillaridin有能力抑制纳+/K+ ATPase酶,导致细胞内钠和钙浓度增加,最终增加心脏萎缩性.这一机制有助于治疗某些心脏病,特别是心脏衰竭和心律失常.该物质还具有潜在的毒性效应,其中可能包括胃肠紊乱和如果滥用心脏心律.由于治疗指数狭窄,Proscillaridin通常在严格的医疗监督下进行.此外,已经研究过其潜在的抗炎和抗癌特性,尽管需要进一步研究以充分了解这些影响.

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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: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-6699676-B1
    优先权日:1999-06-03
    标题:Uses of ouabain and ouabain-like molecules in apoptosis related pathologies
    发明人:ORLOV SERGEI N; HAMET PAVEL; TREMBLAY JOHANNE
    权利人:CORP DU CT DE RECH DU CT HOSPI
    摘要:Longterm elevation of the intracellular Na + /K + ratio inhibits macromolecule synthesis and proliferation in the majority of cell types studied so far, including vascular smooth muscle cells (VSMC). We report here that inhibition of the Na + ,K + pump in VSMC by ouabain or 1 hour preincubation in K + -depleted medium attenuated apoptosis triggered by serum withdrawal, staurosporine or okadaic acid. In the absence of ouabain, both DNA degradation and caspase-3 activation in VSMC undergoing apoptosis were insensitive to modification of the extracellular Na + /K + ratio as well as to hyperosmotic cell shrinkage. In contrast, protection of VSMC from apoptosis by ouabain was abolished under equimolar substitution of Na + o with K + o , showing that the anti apoptotic action of Na + ,K + pump inhibition was caused by inversion of the intracellular Na + /K + ratio. Unlike VSMC, the same level of increment of the [Na + ] i /[K + ] i ratio caused by 2 hours preincubation of Jurkat cells with ouabain did not affect chromatin cleavage and caspase-3 activity triggered by treatment with Fas ligand, staurosporine or hyperosmotic shrinkage. Thus, our results show for the first time that similarly to cell proliferation, maintenance of a physiologically low intracellular Na + /K + ratio is required for progression of VSMC apoptosis.

    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

    专利号:AU-2007308022-A1
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:US-2008107598-A1
    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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    1: Brunetti M, Iasenza IA, Jenner AL, Raynal NJ, Eppert K, Craig M. Mathematical modelling of clonal reduction therapeutic strategies in acute myeloid leukemia. Leuk Res. 2024 May;140:107485. doi: 10.1016/j.leukres.2024.107485. Epub 2024 Mar 16. 13(11):5352-5367.
    3: Jancy SV, Lupitha SS, Chandrasekharan A, Varadarajan SN, Nelson-Sathi S, Prasad R, Jones S, Easwaran S, Darvin P, Sivasailam A, Santhoshkumar TR. A high- throughput screening system for SARS-CoV-2 entry inhibition, syncytia formation and cell toxicity. Biol Proced Online. 2023 Jul 26;25(1):22. doi: 10.1186/s12575-023-00214-1.
    4: Dash UC, Swain SK, Jena AB, Dandapat J, Sahoo AK. The ameliorative effect of Piper trioicum in attenuating cognitive deficit in scopolamine induced neurotoxicity in experimental rats. J Ethnopharmacol. 2024 Jan 10;318(Pt A):116911. doi: 10.1016/j.jep.2023.116911. Epub 2023 Jul 13. 13(1):4685. doi: 10.1038/s41598-023-31276-6.

    合成参考文献


    摘要:Toxicology and Applied Pharmacology., 20(599), 1971 []
    摘要:Drugs in Japan, 6(723), 1982
    摘要:Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology., 62(3)(195S), 1966
    摘要:Arzneimittel-Forschung. Drug Research., 20(1), 1970 []
    摘要:Oyo Yakuri. Pharmacometrics., 2(411), 1968
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