2021 Fiscal Year Final Research Report
Development of biologically active compounds with diversity beyond that of natural compounds
| Project/Area Number |
19H02837
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Review Section |
Basic Section 37020:Chemistry and chemical methodology of biomolecules-related
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| Research Institution | Keio University (2021)
Tohoku University (2019-2020) |
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Principal Investigator |
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| Project Period (FY) |
2019-04-01 – 2022-03-31
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| Keywords | 天然化合物 / 多様性指向型合成 / 生物活性物質 / 多様性拡大抽出物 |
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| Outline of Final Research Achievements |
The diversity-enhanced extracts were utilized as a basic technology to create a group of compounds with diversity beyond that of natural compounds by directly reacting chemical structures that are not incorporated in biosynthesis with extracts from natural resources. Using medicinal plants containing characteristic components as raw materials, we obtained indole alkaloid-type and terpenoid alkaloid-type compounds using non-natural amines, as well as biaryl and biaryl ether/amine-type compounds commonly found in pharmaceutical structures. As a result of extensive bioactivity screening of these compounds, we found bioactive substances that inhibit the expression of immune checkpoint molecules and inhibit osteoclastic differentiation.
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| Free Research Field |
天然物化学
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| Academic Significance and Societal Importance of the Research Achievements |
本研究課題によって得られた成果は，「多様性拡大抽出物」が天然化合物を越える多様性を有した生物活性化合物群を取得するために有用な手法であることを実証したものであり，そのような点で学術的に大いに意義があると言える．一方で，本研究課題によって免疫チェックポイント分子発現阻害作用・破骨細胞分化抑制作用などの生物活性物質が見出され，創薬等への応用可能な分子の創出という点で社会的にも意義のある研究課題であった．
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