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KAKEN_18K14346seika.pdf
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Title |
Title |
海洋天然物由来の抗寄生虫薬リードの創出
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カイヨウ テンネンブツ ユライ ノ コウキセイチュウヤク リード ノ ソウシュツ
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Kaiyō tennenbutsu yurai no kōkiseichūyaku rīdo no sōshutsu
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Investigation of marine natural products for the development of anti-parasite drug leads
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岩崎, 有紘
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イワサキ, アリヒロ
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Iwasaki, Arihiro
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慶應義塾大学・理工学部 (矢上) ・助教
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Research team head
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科研費研究者番号 : 00754897
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野崎, 智義
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ノザキ, トモヨシ
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Nozaki, Tomoyoshi
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Collaborator
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科研費研究者番号 : 60198588
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岩月, 正人
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イワツキ, マサト
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Iwatsuki, Masato
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Collaborator
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科研費研究者番号 : 70353464
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2021
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科学研究費補助金研究成果報告書
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2020
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本研究では、マラリアやトリパノソーマ感染症などの熱帯病の治療に有効な物質を海洋生物から探索した。その結果、22種類の新規天然物を海洋シアノバクテリアから発見し、それらのもつ抗寄生虫活性を明らかにした。さらにこのうち8つの物質について全合成を達成し、供給手段を確立した。特にiheyamideという鎖状ペプチドについては、合成中間体に対する抗寄生虫試験を実施し、構造活性相関を明らかにした。また、iezosideという鎖状ペプチド-ポリケチドハイブリッド化合物については、その作用機序を解明した。
これらの成果については、12報の論文と3報の総説、および34件の学会発表として報告した。
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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研究種目 : 若手研究
研究期間 : 2018~2020
課題番号 : 18K14346
研究分野 : 海洋天然物化学
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