2018 Fiscal Year Final Research Report
Development of biologically active natural product-like compound library based on diversity-enhanced extracts
| Project/Area Number |
16H03279
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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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| Research Field |
Biomolecular chemistry
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| Research Institution | Tohoku University |
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Principal Investigator |
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| Project Period (FY) |
2016-04-01 – 2019-03-31
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| Keywords | 天然物化学 / 多様性指向型合成 / 化合物ライブラリー / メロテルペノイド |
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| Outline of Final Research Achievements |
We proposed a new approach, diversity-enhanced extracts, for increasing the diversity of natural product-like compounds. Diversity-enhanced extracts are prepared from chemical reactions that remodel molecular scaffolds directly on extracts of natural resources. The subsequent isolation of each compound produced from such reactions affords a diverse natural product-like library. Direct, three successive chemical reactions were performed on plant extracts containing a large amount of terpenes to prepare diversity-expanding extracts, which were then separated to give more than 20 kinds of phenolic and pyrone-type merotelpenoids. As a result of carrying out extensive biological activity screening for these compounds, bioactive substances such as osteoclast differentiation inhibitory activity were found.
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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」が構造多様性の高い生物活性を指向した天然化合物類縁体ライブラリーを構築する上で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破骨細胞分化抑制作用などの生物活性物質が見出されたことは，創薬等への応用によって社会への成果還元の可能性をもたらすものであり，社会的にも意義があると言える．
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