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Synthesis of glycosylated derivatives of ginkgolides and in vivo evaluation of those pharmacokinetics

Research Project

Project/Area Number 24590156
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Drug development chemistry
Research InstitutionNational Institute of Radiological Sciences (2013-2014)
The Institute of Physical and Chemical Research (2012)

Principal Investigator

ISHII Hideki  独立行政法人放射線医学総合研究所, 分子イメージング研究センター, 主任研究員 (80425610)

Co-Investigator(Kenkyū-buntansha) KOYAMA Hiroko  岐阜大学, 大学院医学系研究科, 助教 (50402160)
Project Period (FY) 2012-04-01 – 2015-03-31
Project Status Completed (Fiscal Year 2014)
Budget Amount *help
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2014: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2013: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2012: ¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
Keywords天然物 / プロドラック / PET / プローブ / ギンコライド
Outline of Final Research Achievements

It is said that the effect to Alzheimer or dementia of the ginkgo biloba is caused by ginkgolides, but an evaluation halves that because of the low lipophilicity of ginkgolides, the dramatic curative effect were not observed in the most of cases. In order to overcome these problems, we planned the synthesis of glicosylated which might promote the uptake of ginkgolides to the brain through glucose transporter. In addition, we planned that the in vivo dynamics of the ginkgolide derivatives which we designed composed a short-life radionuclide-labeled derivative and evaluated it.

Report

(4 results)
  • 2014 Annual Research Report   Final Research Report ( PDF )
  • 2013 Research-status Report
  • 2012 Research-status Report
  • Research Products

    (4 results)

All 2015 2014 2013 2012

All Journal Article (3 results) (of which Peer Reviewed: 3 results,  Acknowledgement Compliant: 1 results) Presentation (1 results)

  • [Journal Article] Pd(0)-mediated [11C]carbonylation of aryl and heteroaryl boronic acid pinacol esters with [11C]carbon monoxide under ambient conditions and a facile process for the conversion of [carbonyl-11C] esters to [carbonyl-11C]amides2015

    • Author(s)
      Hideki Ishii, Katsuyuki Minegishi, Koutaro Nagatsu, Ming-Rong Zhang
    • Journal Title

      Tetrahedron

      Volume: 71 Issue: 10 Pages: 1588-1596

    • DOI

      10.1016/j.tet.2015.01.008

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Synthesis of 11C-labeled retinoic acid, [11C]ATRA, via an alkenylboron precursor by Pd(0)-mediated rapid C-[11C]methylation2014

    • Author(s)
      Masaaki Suzuki, Misato Takashima-Hirano, Hideki Ishii, Chika Watanabe, Kengo Sumi, Hiroko Koyama, Hisashi Doi,
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 24 Issue: 15 Pages: 3622-3625

    • DOI

      10.1016/j.bmcl.2014.05.041

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis of [11C]Am80 via novel Pd(0)-mediated rapid [11C]carbonylation using aryl-boronate and [11C]carbon monoxide2012

    • Author(s)
      Misato Takashima-Hirano, Hideki Ishii, Masaaki Suzuki
    • Journal Title

      ACS Medicinal Chemistry Letters

      Volume: 3 Issue: 10 Pages: 804-807

    • DOI

      10.1021/ml300160w

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Presentation] Synthesis of 6-deoxy-10-[18F]-Ginkgolide B as a PET probe for in vivo study2013

    • Author(s)
      Hideki Ishii, Hiroshi Mizuma, Hirotaka Onoe, Masaaki Suzuki
    • Organizer
      21st Winter Fluorine Conference
    • Place of Presentation
      St. Pete Beach, Florida (USA)
    • Related Report
      2012 Research-status Report

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Published: 2013-05-31   Modified: 2019-07-29  

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