| Project/Area Number |
17K19191
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| Research Category |
Grant-in-Aid for Challenging Research (Exploratory)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Biomolecular chemistry and related fields
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| Research Institution | Chiba University |
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Principal Investigator |
Arai Midori 千葉大学, 大学院薬学研究院, 准教授 (40373261)
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| Project Period (FY) |
2017-06-30 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥6,500,000 (Direct Cost: ¥5,000,000、Indirect Cost: ¥1,500,000)
Fiscal Year 2018: ¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
Fiscal Year 2017: ¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
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| Keywords | 天然物 / 光環化反応 / ロカグラミド / Wnt / がん / ライブラリー / 光環化付加反応 / Wntシグナル / 阻害剤 / 光環化付加 / 植物エキス / 多様性 / 天然物化学 / 光反応 / エキス |
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| Outline of Final Research Achievements |
Extract of natural resources is a mixture of unknown diversified natural products. In this research, we aimed the synthesis of new natural products mixture by photo-cyclized reaction. Although several MeOH extracts of plants were irradiated by UV lamp with olefin compounds, unfortunately reproducibility was low. Therefore, synthesis of rocaglamides with fluorous tag was examined. We also succeeded in synthesizing of rocaglamide derivatives with heterocycles. They showed strong Wnt signal inhibitory activity. Moreover, biotin-tagged rocaglamides retained the Wnt signal inhibitory activity.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究では生薬エキスを用いて光環化付加反応を検討した．光反応を用いたエキス有機合成は初の試みであった．また，光環化付加反応を用いて種々のヘテロ環ロカグラミド誘導体の合成に成功し，それらが，がんで異常亢進しているWntシグナルに対する阻害作用を有していることを見いだした．この結果は，ヘテロ環含有ロカグラミドの新規生物活性を見いだした学術的意義もさることながら，ロカグラミド誘導体が新規抗がん剤リードになる可能性を示唆しており，社会的意義があるものと考えている．
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