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Search for seeds of drugs for tropical diseases from Kitasato microbial library

Research Project

Project/Area Number 17K08343
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Natural medicines
Research InstitutionKitasato University

Principal Investigator

Iwatsuki Masato  北里大学, 感染制御科学府, 准教授 (70353464)

Project Period (FY) 2017-04-01 – 2020-03-31
Project Status Completed (Fiscal Year 2019)
Budget Amount *help
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2019: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2018: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2017: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Keywordsマラリア / リーシュマニア / 微生物代謝産物 / 天然物化学 / 微生物創薬 / 新規化合物 / 糸状菌代謝産物 / 新規ペプチド化合物 / 抗生物質 / リーシュマニア症
Outline of Final Research Achievements

In this project, we successfully discovered six new antimalarial compounds form 3 different fungal cultured broths. From the cultured broth of FKI-7019 strain, we isolated two new linear lipopeptides named kozupeptins A and B, having potent in vitro and in vivo antimalarial activity. From the cultured broth of strain A, we found two new cyclic tetrapeptides showing moderate in vitro antimalarial activity. From the cultured broth of strain B, we found two new heterocyclic compounds displaying moderate in vitro antimalarial activity. We also picked up three known compounds as antileishmanial agents active against Leishmania major in vitro.

Academic Significance and Societal Importance of the Research Achievements

得られた創薬シード化合物は熱帯病治療薬の開発に特化した非営利団体の支援および製薬企業との共同研究によって国際的な開発研究へと展開していくことで各原虫症治療薬の開発に繋がることが期待される。開発された治療薬はマラリアおよびリーシュマニア症による人的被害を軽減することで開発途上国の保健衛生の向上に繋がり、人類の福祉として国際貢献をするものである。

Report

(4 results)
  • 2019 Annual Research Report   Final Research Report ( PDF )
  • 2018 Research-status Report
  • 2017 Research-status Report
  • Research Products

    (9 results)

All 2019 2018 2017

All Journal Article (1 results) (of which Peer Reviewed: 1 results) Presentation (7 results) (of which Int'l Joint Research: 1 results) Patent(Industrial Property Rights) (1 results)

  • [Journal Article] Kozupeptins, Antimalarial Agents Produced by Paracamarosporium Species: Isolation, Structural Elucidation, Total Synthesis, and Bioactivity2019

    • Author(s)
      Hayashi Yumi、Fukasawa Wataru、Hirose Tomoyasu、Iwatsuki Masato、Hokari Rei、Ishiyama Aki、Kanaida Masahiro、Nonaka Kenichi、Take Akira、Otoguro Kazuhiko、Omura Satoshi、Shiomi Kazuro、Sunazuka Toshiaki
    • Journal Title

      Organic Letters

      Volume: 21 Issue: 7 Pages: 2180-2184

    • DOI

      10.1021/acs.orglett.9b00483

    • Related Report
      2018 Research-status Report
    • Peer Reviewed
  • [Presentation] 微生物培養液からの抗マラリア活性害物質の探索 (1)2019

    • Author(s)
      林裕美, 渡邊善洋, 廣瀬 友靖, 深澤航, 岩月正人, 石山亜紀, 穗苅玲, 野中健一, 大村智, 砂塚敏明
    • Organizer
      日本熱帯医学会(第60回)
    • Related Report
      2019 Annual Research Report
  • [Presentation] 微生物培養液からの抗マラリア活性害物質の探索 (2)2019

    • Author(s)
      大内孝仁, 渡邊善洋, 荒川 絵美, 岩月正人, 石山亜紀, 穗苅玲, 松本厚子、野中健一, 大村智
    • Organizer
      日本熱帯医学会(第60回)
    • Related Report
      2019 Annual Research Report
  • [Presentation] 3.New antimalarial compounds from Kitasato microbial cultured broth libraries2019

    • Author(s)
      Masato Iwatsuki, Yumi Hayashi, Wataru Fukasawa, Tomoyasu Hirose, Rei Hokari, Aki Ishiyama, Ken Nonaka, Kazuro Shiomi, Toshiaki Sunazuka, and Satoshi Omura
    • Organizer
      The Joint Symposium of "10th Korea-Japan Chemical Biology Symposium" & "30th Meeting for New Drug Discovery"
    • Related Report
      2019 Annual Research Report
  • [Presentation] 抗マラリア活性を有するkozupeptin類の単離、 構造決定、全合成および活性評価2019

    • Author(s)
      林裕美、廣瀬友靖、深澤航、岩月正人、穂苅玲、石山亜紀、野中健一、塩見和朗、大村智、砂塚敏明
    • Organizer
      第61回天然有機化合物討論会
    • Related Report
      2019 Annual Research Report
  • [Presentation] 新規抗マラリア活性リポペプチド Kozupeptin A の実用的全合成および絶対立体構造の決定2018

    • Author(s)
      林 裕美, 廣瀬 友靖, 深澤 航, 岩月 正人, 野中 健一, 穂苅 玲, 石山 亜紀, 塩見 和朗, 大村 智, 砂塚 敏明
    • Organizer
      日本薬学会 第139回年会
    • Related Report
      2018 Research-status Report
  • [Presentation] New Antimalarial Lipopeptides Produced by Paracamarospurium Species: Isolation, Structural Elucidation, Efficient Total Synthesis, and Biological Activity2018

    • Author(s)
      Yumi Hayashi, Tomoyasu Hirose, Wataru Fukasawa, Masato Iwatsuki, Kenichi Nonaka, Rei Hokari, Aki Ishiyama, Kazuro Shiomi, Satoshi Omura, Toshiaki Sunazuka
    • Organizer
      The 14th International Kyoto Conference on New Aspects of Organic Chemistry (IKCOC-14)
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research
  • [Presentation] 糸状菌が生産する新規抗マラリア活性物質2017

    • Author(s)
      深澤航、森菜月、岩月正人、野中健一、廣瀬友靖、石山亜紀、穂苅玲、乙黒一彦、大村智、塩見和朗
    • Organizer
      第10回 北里化学シンポジウム
    • Related Report
      2017 Research-status Report
  • [Patent(Industrial Property Rights)] 新規FKI-7019物質およびその製造方法2018

    • Inventor(s)
      大村智 乙黒一彦 岩月正人 石山亜紀 穗苅玲 砂塚敏明 他5名
    • Industrial Property Rights Holder
      大村智 乙黒一彦 岩月正人 石山亜紀 穗苅玲 砂塚敏明 他5名
    • Industrial Property Rights Type
      特許
    • Filing Date
      2018
    • Related Report
      2018 Research-status Report

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Published: 2017-04-28   Modified: 2021-02-19  

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