CAS: 64480-66-6; Glycoursodeoxycholic Acid

该化合物是一种可溶酸的酸衍生物,在肠胃中吸收脂肪和脂肪溶解的维生素,在消化和吸收过程中发挥作用;是一种由聚氧氧氧基酸与甘油结合而形成的同卵二恶英酸,是一种同卵二恶英酸,这种复合物具有亚虫性,即它既具有水利性,又具有缺水性,有助于它在脂质乳化过程中发挥洗涤剂作用;众所周知,甘醇代氧基酸具有潜在的治疗作用,特别是在肝病治疗和胆石溶解过程中,它也可能具有保护性,有助于保护肝细胞不受损害;在溶解性方面,由于极地功能组,它通常在水中溶解.其分子结构包括一种具有盐质的脊椎,其中含有有助于其生物活动的盐质组.

结构式图片

上下游产品

chenodeoxycholic acid 3α,7α-dihydroxy-5β-cholan-24-oic acid 2,5-dioxopyrrolidin-1-yl ester glycine ursodeoxycholic acid ethyl ester glycine

合成工艺路线路线简述

    熊去氧胆酸置于盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺,聚甘氨酸体系中,用 二氯甲烷,二甲基亚砜 作为反应溶剂,化学反应 8.0H,反应生成 甘氨熊去氧胆酸
    参考文献:Synthesis,Anticancer Activities,Antimicrobial Activities And Bioavailability Of Berberine-Bile Acid Analogues
    标题:Synthesis,Anticancer Activities,Antimicrobial Activities And Bioavailability Of Berberine-Bile Acid Analogues
    摘要:合成了十五种小檗碱-胆酸类似物.与小檗碱(bbr)相比,这些类似物的抗癌活性在体外进行了评估;在这些类似物中,A4,B4 和 B5 的细胞毒性高于 Bbr.大多数类似物对金黄色葡萄球菌 Atcc 25923 和白色念珠菌 Atcc 8799 具有较高的抗菌活性,而对枯草芽孢杆菌 As 1.398 和大肠杆菌 Atcc 31343 则无敏感性.a4 和 B4 在血清稳定性实验中表现出稳定性.b4 在小鼠中显示出非常好的口服生物利用度.
    DOI:10.2174/157018012800673010

    海关参考信息

    专利信息


    专利号:WO-2020020904-A1
    优先权日:2018-07-23
    标题:Therapeutic uses of glp-2 agonists
    发明人:LINDSTRÖM ERIK; SKARBALIENE JOLANTA
    权利人:ZEALAND PHARMA AS
    摘要:The invention relates to the use of GLP-2 agonists to modulate bile acid metabolism. In particular, it is believed that GLP-2 agonists may be capable of inhibiting bile acid synthesis, and so are useful for the treatment of conditions in which inhibition of bile acid synthesis is beneficial. Such conditions include primary bile acid diarrhea, secondary bile acid diarrhea and conditions which cause or contribute to cholestasis. The invention further relates to the use of FGF19 and C4 as biomarkers to monitor bile acid synthesis and homoeostasis, e.g. in SBS patients.

    专利号:US-2012232169-A1
    优先权日:2011-03-07
    标 题 :Highly monodisperse branched peg-lipid conjugates
    发明人:WU NIAN; KELLER BRIAN CHARLES
    权利人:WU NIAN; KELLER BRIAN CHARLES; BIOZONE PHARMACEUTICALS INC
    摘要:(PEG)-lipid conjugates and methods of preparation are disclosed herein. Methods of preparation may involve stepwise addition of small PEG oligomers to a glycerol backbone until a desired chain size is attained. Polymers resulting from the syntheses may be highly monodisperse. The resulting polymers may comprise branched polyethyleneglycol (PEG)-lipid conjugates. The present disclosure may provide several advantages such as simplified synthesis, high product yield and low cost for starting materials. The present synthesis method may be suitable for preparing a wide range of conjugates such as PEG lipid conjugates having a glycerol-like central backbone covalently attached to two or more monodisperse PEG chains and a lipid comprising a range of diesters made from fatty acids or bile acids.

    专利号:US-2011040113-A1
    优先权日:2009-06-02
    标 题 :Pure PEG-lipid conjugates
    发明人:WU NIAN; KELLER BRIAN CHARLES
    权利人:WU NIAN; KELLER BRIAN CHARLES
    摘要:Syntheses of polyethyleneglycol (PEG)-lipid conjugates are disclosed. Such syntheses involve stepwise addition of small PEG oligomers to a glycerol backbone until the desired chain size is attained. Polymers resulting from the syntheses are highly monodisperse. The present invention provides several advantages such as simplified synthesis, high product yield and low cost for starting materials. The present synthesis method is suitable for preparing a wide range of conjugates. n In another aspect, the invention comprises PEG lipid conjugates having a glycerol backbone covalently attached to one or two monodisperse PEG chains and one or two lipids. These conjugates are especially useful for pharmaceutical formulations.
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    主要参考文献


    1: Sun L, Xie C, Wang G, Wu Y, Wu Q, Wang X, Liu J, Deng Y, Xia J, Chen B, Zhang S, Yun C, Lian G, Zhang X, Zhang H, Bisson WH, Shi J, Gao X, Ge P, Liu C, Krausz KW, Nichols RG, Cai J, Rimal B, Patterson AD, Wang X, Gonzalez FJ, Jiang C. Gut microbiota and intestinal FXR mediate the clinical benefits of metformin. Nat Med. 2018 Dec;24(12):1919-1929. doi: 10.1038/s41591-018-0222-4. Epub 2018 Nov 5.
    2: Van den Bossche L, Hindryckx P, Devisscher L, Devriese S, Van Welden S, Holvoet T, Vilchez-Vargas R, Vital M, Pieper DH, Vanden Bussche J, Vanhaecke L, Van de Wiele T, De Vos M, Laukens D. Ursodeoxycholic Acid and Its Taurine- or Glycine-Conjugated Species Reduce Colitogenic Dysbiosis and Equally Suppress Experimental Colitis in Mice. Appl Environ Microbiol. 2017 Mar 17;83(7):e02766-16. doi: 10.1128/AEM.02766-16.
    3: Goldman A, Condon A, Adler E, Minnella M, Bernstein C, Bernstein H, Dvorak K. Protective effects of glycoursodeoxycholic acid in Barrett's esophagus cells. Dis Esophagus. 2010 Feb;23(2):83-93. doi: 10.1111/j.1442-2050.2009.00993.x. Epub 2009 Jun 22. 71(3):893-906. doi: 10.1002/hep.30852. Epub 2019 Aug 19. 51(3):864-77. doi: 10.1007/s12035-014-8731-8. Epub 2014 May 22.

    合成参考文献


    参考文献:10.1016/j.jchromb.2008.04.045
    摘要:Bentayeb K, Batlle R, Sánchez C, Nerín C, Domeño C. Determination of bile acids in human serum by on-line restricted access material-ultra high-performance liquid chromatography-mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jun 15;869(1-2):1–8. doi: 10.1016/j.jchromb.2008.04.045.
    参考文献:10.1002/hep.20961
    摘要:Ballatori N, Christian WV, Lee JY, Dawson PA, Soroka CJ, Boyer JL, Madejczyk MS, Li N. OSTalpha-OSTbeta: a major basolateral bile acid and steroid transporter in human intestinal, renal, and biliary epithelia. Hepatology. 2005 Dec;42(6):1270–9. doi: 10.1002/hep.20961.
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