| Project/Area Number |
18K14346
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| Research Category |
Grant-in-Aid for Early-Career Scientists
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| Allocation Type | Multi-year Fund |
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| Review Section |
Basic Section 37020:Chemistry and chemical methodology of biomolecules-related
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| Research Institution | Keio University |
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Principal Investigator |
Iwasaki Arihiro 慶應義塾大学, 理工学部(矢上), 助教 (00754897)
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| Project Period (FY) |
2018-04-01 – 2021-03-31
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| Project Status |
Completed (Fiscal Year 2020)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2020: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2019: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
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| Keywords | 天然物化学 / シアノバクテリア / ペプチド / トリパノソーマ / マラリア / 寄生虫 / 熱帯病 / 海洋天然物 / 抗寄生虫薬 / 海洋天然物化学 / 作用機序解明 |
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| Outline of Final Research Achievements |
In this research project, I investigated new natural products possessing useful biological activities for the treatment of tropical diseases, such as malaria and trypanosomiasis, from marine organisms. As a result, I found twenty-two new natural products from marine cyanobacteria and clarified their anti-parasite activities. In addition, I achieved the total synthesis of eight compounds out of them and established supply routes for those precious natural products. Especially among them, I evaluated anti-parasite activities of several synthetic intermediates of iheyanone, an acyclic peptide, and clarified its structure-activity relationship. Furthermore, I established the mode of action of the biological activity of an acyclic peptide-polyketide hybrid compound, iezoside.
These results were reported as twelve scientific papers, three reviews, and thirty-four presentations in academic meetings.
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| Academic Significance and Societal Importance of the Research Achievements |
マラリア原虫やトリパノソーマ原虫が引き起こす感染症は、アフリカや南米の発展途上国を中心にまん延している。患者の多くが貧困層であるため、製薬会社は新薬の開発に消極的で、効果や安全性に問題がある古い薬が使われ続けている。
本研究は、こうした感染症の治療に効果がある物質を海洋生物から発見することを目指し、結果として22種類の新しい物質の発見に成功した。こうした物質の多くは、ヒトの細胞に毒性をしめす濃度よりも低濃度で寄生虫の増殖を抑えたことから、新しい抗寄生虫薬の開発のヒントになると期待される。さらに、こうした物質の化学合成法の開発や、作用メカニズムの解明を行った。
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