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2013 Fiscal Year Final Research Report

Development of novel pro-drugs based on the bile acid as a core compound

Research Project

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Project/Area Number 23590209
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Medical pharmacy
Research InstitutionKinki University

Principal Investigator

MITAMURA Kuniko  近畿大学, 薬学部, 准教授 (70242526)

Co-Investigator(Kenkyū-buntansha) IKEGAWA Shigeo  近畿大学, 薬学部, 教授 (90111301)
Project Period (FY) 2011 – 2013
Keywords胆汁酸 / N-アセチルシステイン / プロドラッグ / 肝・胆・消化機能改善薬 / 液体クロマトグラフィー / 質量分析法
Research Abstract

We demonstrated that N-acetylcysteine conjugate of ursodeoxycholic acid (UDCA-NAC) was hydrolyzed and circulated in body as UDCA after administration by injection via jugular vein, while UDCA-NAC converted to NAC-sulfate di-conjugate by rat liver cytosolic fraction. Furthermore, UDCA-NAC was shown to inhibit the increase of liver disease marker enzymes, AST and ALT, in serum of acetaminophen-induced liver injury rats. These results showed that UDCA-NAC is useful as a prodrug of the new liver, bile, digestive function improving agent.

  • Research Products

    (20 results)

All 2014 2013 2012 2011

All Journal Article (8 results) (of which Peer Reviewed: 7 results) Presentation (10 results) Book (2 results)

  • [Journal Article] Simultaneous determination of 18 tetrahydrocor- ticosteroid sulfates in human urine by liquid chromatography/electrospray ionization-tandem mass spectrometry2014

    • Author(s)
      Mitamura K, Satoh (née Okihara) R, Kamibayashi M, Sato K, Iida T, Ikegawa S
    • Journal Title

      Steroids

      Volume: 85 Pages: 18-29

    • DOI

      10.1016/j.steroids.2014.03.015

    • Peer Reviewed
  • [Journal Article] N-Methyltaurine N-acyl amidated bile acids and deoxycholic acid in the bile of angelfish (Pomacanthidae): A novel bile acid profile in Perciform fish2013

    • Author(s)
      Satoh (née Okihara) R, Saito T, Ogata H, Ohsaki A, Iida T, Asahina K, Mitamura K, Ikegawa S, Hofmann AF, Hagey LR
    • Journal Title

      Steroids

      Volume: 80 Pages: 15-23

    • DOI

      10.1016/j.steroids.2013.11.014

    • Peer Reviewed
  • [Journal Article] MS解析でわかる胆汁酸の世界2012

    • Author(s)
      三田村邦子, 東達也, 池川繁男
    • Journal Title

      分子消化器病

      Volume: 9 Pages: 273-278

  • [Journal Article] A novel varanic acid epimer—(24R, 25S)-3α,7α,12α,24-tetrahydroxy-5β- cholestan- 27-oic acid—is a major biliary bile acid in two varanid lizards and the Gila monster2012

    • Author(s)
      Hagey LR, Ogawa S, Kato N, Satoh née Okihara R, Une M, Mitamura K, Ikegawa S, Hofmann AF, Iida T
    • Journal Title

      Steroids

      Volume: 77 Pages: 1510-1521

    • DOI

      10.1016/j.steroids.2012.08.017

    • Peer Reviewed
  • [Journal Article] Synthesis of the 3-sulfates of S-acyl glutathione conjugated bile acids and their biotransformation by a rat liver cytosolic fraction2012

    • Author(s)
      Mitamura K, Hori N, Mino S. Iida T, Hofmann AF, Ikegawa S
    • Journal Title

      Chem. Phys. Lipids

      Volume: 165 Pages: 261-269

    • DOI

      10.1016/j.chemphyslip.2012.02.001

    • Peer Reviewed
  • [Journal Article] Identification of S-acyl glutathione conjugates of bile acids in human bile by means of LC/ESI-MS2011

    • Author(s)
      Mitamura K, Hori N, Iida T, Suzuki M, Shimizu T, Nittono H, Takaori K, Takikawa H, Honmann AF, Ikegawa S
    • Journal Title

      Steroids

      Volume: 76 Pages: 1609-1614

    • DOI

      10.1016/j.steroids.2011.10.001

    • Peer Reviewed
  • [Journal Article] Characterization of non-enzymatic acylation of amino or thiol groups of bionucleophiles by the acyl-adenylate or acyl-CoA thioester of cholic acid2011

    • Author(s)
      Mitamura K, Aoyama E, Sakai T, Iida T, Hofmann AF, Ikegawa S
    • Journal Title

      Anal. Bioanal. Chem

      Volume: 400 Pages: 2253-2259

    • DOI

      10.1007/s00216-011-4961-z

    • Peer Reviewed
  • [Journal Article] Synthesis of the 3-sulfates of N-acetylcysteine conjugated bile acids (BA-NACs) and their transient formation from BA-NACs and subsequent hydrolysis by a rat liver cytosolic fraction as shown by liquid chromatography/electrospray ionization-mass spectrometry2011

    • Author(s)
      Mitamura K, Sakai T, Nakai R, Wakamiya T, Iida T, Hofmann AF, Ikegawa S
    • Journal Title

      Ana.l Bioanal. Chem

      Volume: 400 Pages: 2061-2072

    • DOI

      10.1007/s00216-011-4925-3

    • Peer Reviewed
  • [Presentation] ピラルクー(Arapaima gigas)の胆嚢胆汁から新規胆汁酸タウリン抱合体の単離と構造決定2014

    • Author(s)
      齊藤徹也
    • Organizer
      日本薬学会第134年会
    • Place of Presentation
      熊本市総合体育館(熊本市)
    • Year and Date
      20140328-30
  • [Presentation] 尿中ステロイドのLC-MS/MS2013

    • Author(s)
      三田村邦子
    • Organizer
      第60回日本臨床検査医学会学術集会
    • Place of Presentation
      神戸国際会議場(神戸市)
    • Year and Date
      20131101-05
  • [Presentation] Barrett食道患者の胃液内胆汁酸の解析2013

    • Author(s)
      池川繁男
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      パシフィコ横浜(横浜市)
    • Year and Date
      20130328-30
  • [Presentation] Identification of S-acyl glutathione conjugates of bile acids in human bile by means of LC/ESI-MS2012

    • Author(s)
      Ikegawa S
    • Organizer
      XXII Bile Acid Meeting
    • Place of Presentation
      Hilton Vienna Hotel (Vienna, Austria)
    • Year and Date
      20121015-16
  • [Presentation] 安定同位体希釈LC/ESI-MS/MSによる尿中グルタミン抱合型胆汁酸の高感度測定法の開発2012

    • Author(s)
      池川繁男
    • Organizer
      第52回臨床化学会年次学術集会
    • Place of Presentation
      岩手県民情報センター(盛岡市)
    • Year and Date
      20120906-08
  • [Presentation] Liquid chromatography-mass spectrometric characterization of sulfation of glutathione conjugated bile acids by a rat liver cytosolic fraction2012

    • Author(s)
      Ikegawa S
    • Organizer
      60th ASMS Conference on Mass Spectrometry and Allied Topics
    • Place of Presentation
      Vancouver Convention Center (Vancouver, Canada)
    • Year and Date
      20120520-24
  • [Presentation] グルタミン抱合型胆汁酸の合成とそれらのESI-MSにおける挙動2012

    • Author(s)
      池川繁男
    • Organizer
      第62回日本薬学会近畿支部総会・大会
    • Place of Presentation
      武庫川女子大(西宮市)
    • Year and Date
      2012-10-20
  • [Presentation] LC/MSによるグルタチオン抱合型胆汁酸の動態解析2011

    • Author(s)
      三田村邦子
    • Organizer
      第60回日本分析化学会
    • Place of Presentation
      名古屋大学(名古屋市)
    • Year and Date
      2011-09-05
  • [Presentation] N-アセチルシステイン抱合型ウルソデオキシコール酸の体内動態と肝機能改善作用に関する基礎的検討2011

    • Author(s)
      三田村邦子
    • Place of Presentation
      リーガロイヤルホテル大阪(大阪市)
    • Year and Date
      2011-07-23
  • [Presentation] グルタチオン抱合型胆汁酸3-サルフェートの合成とラット肝サイトゾール画分における生成2011

    • Author(s)
      三田村邦子
    • Organizer
      第28回日本胆膵病態生理研究会
    • Place of Presentation
      福大メディカルホール(福岡市)
    • Year and Date
      2011-06-18
  • [Book] 試料分析講座脂質分析2011

    • Author(s)
      池川繁男、三田村邦子
    • Total Pages
      135-148
    • Publisher
      丸善
  • [Book] 分析化学便覧2011

    • Author(s)
      東達也、三田村邦子
    • Total Pages
      389-392
    • Publisher
      丸善

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Published: 2015-07-16  

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