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2012 Fiscal Year Final Research Report

Search for new antitumor lead-compounds originated from plant alkaloids

Research Project

  • PDF
Project/Area Number 22510224
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Living organism molecular science
Research InstitutionChiba University

Principal Investigator

KITAJIMA Mariko  千葉大学, 大学院・薬学研究院, 准教授 (60195261)

Project Period (FY) 2010 – 2012
Keywords天然物化学 / 生物活性物質
Research Abstract

To discover and develop lead-compounds for new antitumor medicines originated from plant alkaloids, chemical investigation and biological evaluation of Gelsemium alkaloids and colchicinoids were carried out. As results, several novel alkaloids were isolated from Gelsemium plants. Key intermediates of sarpagine-type alkaloids, one of the members of Gelsemium alkaloids, were synthesized utilizing gold-catalyzed cyclization. 4-Halocolchicines and 4-chlorocolchicine derivatives bearing anα-hydroxyacetoamide side chain at C-7 were found to show potent antitumor activities. Pro-drugs of highly-active colchicine derivatives were prepared and their selective toxicity to the tumor cells was evaluated.

  • Research Products

    (25 results)

All 2013 2012 2011 2010 Other

All Journal Article (5 results) (of which Peer Reviewed: 5 results) Presentation (17 results) Remarks (1 results) Patent(Industrial Property Rights) (2 results) (of which Overseas: 1 results)

  • [Journal Article] Seven New Monoterpenoid Indole Alkaloids from Gelsemium elegans2011

    • Author(s)
      Y. Yamada, M. Kitajima, N. Kogure, S. Wongseripipatana, and H. Takayama
    • Journal Title

      Chem. Asian J

      Volume: 6 Pages: 166-173

    • DOI

      DOI:10.1002/asia.201000538.

    • Peer Reviewed
  • [Journal Article] Design, Synthesis, and Antitumor Activity of 4-Halocolchicines and their Pro-drugs Activated by Cathepsin B2011

    • Author(s)
      N. Yasobu, M. Kitajima, N. Kogure, Y. Shishido, T. Matsuzaki, M. Nagaoka, and H. Takayama
    • Journal Title

      ACS Med. Chem. Lett

      Volume: 2 Pages: 348-352

    • DOI

      DOI:10.1021/m1100287y.

    • Peer Reviewed
  • [Journal Article] Metacolchicine, A New Colchicinoid from Sandersonia aurantiaca2011

    • Author(s)
      M. Kitajima, A. Tanaka, N. Kogure, and H. Takayama
    • Journal Title

      Heterocycles

      Volume: 83 Pages: 1903-1907

    • Peer Reviewed
  • [Journal Article] Synthesis and Biological Evaluation of Indole Alkaloids from Gelsemiumrankinii2010

    • Author(s)
      H. Nishiyama, M. Ono, T. Sugimoto, T.Sasai, N. Asakawa, T. Matsumoto, T. Yaegashi, M. Nagaoka, T. Matsuzaki, N. Kogure, M. Kitajima, and H. Takayama
    • Journal Title

      Tetrahedron

      Volume: 66 Pages: 5987-5992

    • DOI

      DOI:10.1016/j.tet.2010.06.032.

    • Peer Reviewed
  • [Journal Article] New Oxindole and Indole Alkaloids from Gelsemium rankinii2010

    • Author(s)
      M. Kitajima, H. Kobayashi, N. Kogure, and H. Takayama
    • Journal Title

      Tetrahedron

      Volume: 66 Pages: 5987-5992

    • DOI

      DOI:10.1016/j.tet.2010.06.032.

    • Peer Reviewed
  • [Presentation] 腫瘍細胞選択性を有するコルヒチン系ダブルプロドラッグ化合物の合成研究2013

    • Author(s)
      遠藤慎平,八十歩直子,北島満里子,小暮紀行,高山廣光
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      横浜
    • Year and Date
      2013-03-29
  • [Presentation] がん細胞選択毒性を有するColchicine系抗腫瘍薬の創製研究2012

    • Author(s)
      北島満里子,八十歩直子,小暮紀行,宍戸祐之,松崎健,長岡正人,高山廣光
    • Organizer
      第54回天然有機化合物討論会
    • Place of Presentation
      東京
    • Year and Date
      2012-09-19
  • [Presentation] 新規colchicine誘導体を利用した腫瘍細胞選択的プロドラッグ化合物の創製研究2012

    • Author(s)
      八十歩直子,北島満里子,小暮紀行,宍戸祐之,松崎健,長岡正人,高山廣光
    • Organizer
      日本薬学会第132年会
    • Place of Presentation
      札幌
    • Year and Date
      2012-03-30
  • [Presentation] New Monoterpenoid Indole Alkaloids from Gelsemium elegans2011

    • Author(s)
      N. Kogure, Y. Yamada, M. Kitajima, S.Wongseripipatana and H. Takayama
    • Organizer
      The 6^<th> International Conference on Cutting-Edge Organic Chemistry in Asia and 2^<nd> New Phase International Conference on Cutting-Edge Organic Chemistry in Asia (ICCEOCA-6/NICCEOCA-2)
    • Place of Presentation
      HongKong, China
    • Year and Date
      2011-12-12
  • [Presentation] Isolation, Structure Elucidaiton, Chemical Transformation and Biological Evaluation of Novel Gelsemium Alkaloids2011

    • Author(s)
      Y. Yamada, M. Kitajima, N. Kogure, S.Wongseripipatana, and H. Takayama
    • Organizer
      8th AFMC International Medicinal Chemistry Symposium (AIMECS11)
    • Place of Presentation
      Tokyo
    • Year and Date
      2011-11-30
  • [Presentation] Synthesis of4-Halocolchicines and Their Pro-drugDerivatives having Potent Antitumor Activity2011

    • Author(s)
      N. Yasobu, M. Kitajima, N. Kogure, Y.Shishido, T. Matsuzaki, M. Nagaoka, and H. Takayama
    • Organizer
      8th AFMC International Medicinal Chemistry Symposium (AIMECS11)
    • Place of Presentation
      Tokyo
    • Year and Date
      2011-11-30
  • [Presentation] アカネ科Ophiorrhiza trichocarpon含有新規インドールアルカロイド配糖体の構造解析2011

    • Author(s)
      北島満里子,尾原聡子,小暮紀行,Dammrong Santiarworn,高山廣光
    • Organizer
      第53回天然有機化合物討論会
    • Place of Presentation
      大阪
    • Year and Date
      2011-09-27
  • [Presentation] Gelsemium elegans含有新規アルカロイドの成分探索および化学的研究2011

    • Author(s)
      山田洋介,小暮紀行,北島満里子,高山廣光,Sumphan Wongseripipatana
    • Organizer
      日本生薬学会第58回年会シンポジウム
    • Place of Presentation
      東京
    • Year and Date
      2011-09-24
  • [Presentation] 薬用資源植物含有生物活性アルカロイドの探索と創薬先導化合物の創製研究2011

    • Author(s)
      北島満里子
    • Organizer
      第28回和漢医薬学会学術大会シンポジウム
    • Place of Presentation
      富山
    • Year and Date
      2011-08-27
  • [Presentation] Colchicine誘導体を基盤としたプロドラッグ化合物の創製研究2011

    • Author(s)
      八十歩直子,北島満里子,小暮紀行,高山廣光
    • Organizer
      第46回天然物化学談話会
    • Place of Presentation
      熱川
    • Year and Date
      2011-07-07
  • [Presentation] Sempervirine誘導体の合成研究2011

    • Author(s)
      山田洋介,小暮紀行,北島満里子,高山
    • Organizer
      第46回天然物化学談話会
    • Place of Presentation
      熱川
    • Year and Date
      2011-07-07
  • [Presentation] ゲルセミウムアルカロイドSempervirineをシードとした抗腫瘍薬の創製研究-1-2011

    • Author(s)
      山田洋介,北島満里子,小暮紀行,高山廣光
    • Organizer
      日本薬学会第131年会
    • Place of Presentation
      静岡
    • Year and Date
      2011-03-31
  • [Presentation] 新規colchicine誘導体を利用したプロドラッグ化合物の創製2011

    • Author(s)
      八十歩直子,北島満里子,小暮紀行,宍戸祐之,松崎健,長岡正人,高山廣光
    • Organizer
      日本薬学会第131年会
    • Place of Presentation
      静岡
    • Year and Date
      2011-03-29
  • [Presentation] Isolation, Spectroscopic analyses, Chemical Transformation and Biological Evaluation of Novel Gelsemium Alkaloids2010

    • Author(s)
      Y. Yamada, M. Kitajima, N. Kogure, S.Wongseripipatana, H. Takayama
    • Organizer
      2010 International Chemical Congress of Pacific Basin Societies (PACIFICHEM2010)
    • Place of Presentation
      Hawaii, USA
    • Year and Date
      2010-12-18
  • [Presentation] がん細胞選択毒性を有するcolchicine系抗腫瘍薬の創製研究2010

    • Author(s)
      八十歩直子,小暮紀行,北島満里子,松崎健,長岡正人,高山廣光
    • Organizer
      第29回メディシナルケミストリーシンポジウム
    • Place of Presentation
      京都
    • Year and Date
      2010-11-17
  • [Presentation] ゲルセミ2010

    • Author(s)
      山田洋介,北島満里子,小暮紀行,小林宏美,石井直子,Sumphan Wongseripipatana,高山廣光
    • Organizer
      第52回天然有
    • Place of Presentation
      静岡
    • Year and Date
      2010-10-01
  • [Presentation] Novel Monoterpenoid Indole Alkaloids from Gelsemium elegans2010

    • Author(s)
      Y. Yamada, M. Kitajima, N. Kogure, S.Wongseripipatana, H. Takayama
    • Organizer
      The 57^<th> Annual Meeting of the Japanese Society of Pharmacognosy (Tokushima, 2010), and The 5th JSP-CCTNM-KSP Joint Symposium on Pharmacognosy
    • Place of Presentation
      Tokushima
    • Year and Date
      2010-09-24
  • [Remarks]

    • URL

      http://www.p.chiba-u.ac.jp/lab/seitai/index.html

  • [Patent(Industrial Property Rights)] Colchicine Derivatives2011

    • Inventor(s)
      H. Takayama et al.
    • Industrial Property Rights Holder
      千葉大学 他
    • Industrial Property Number
      PCT Int. Appl.WO 2011021397
    • Filing Date
      2011-02-24
    • Overseas
  • [Patent(Industrial Property Rights)] コルヒチン誘導体2010

    • Inventor(s)
      高山廣光, 他
    • Industrial Property Rights Holder
      千葉大学 他
    • Industrial Property Number
      出願PCT/JP2010/005136
    • Filing Date
      2010-08-20

URL: 

Published: 2014-08-29  

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