Structure-activity relationship study on the tumor angiogenesis inhibition activity of fucoidan
| Project/Area Number |
18K05455
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 38040:Bioorganic chemistry-related
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| Research Institution | Gifu University |
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Principal Investigator |
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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 |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2020: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2019: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2018: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | フコイダン / 糖鎖 / 有機合成 / 立体選択的グリコシル化 / 化学合成 / 構造活性相関 / 血管新生 / 硫酸化多糖 |
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| Outline of Final Research Achievements |
We have developed a unique synthetic method for natural fucoidan molecules. Based on the fact that L-fucose is 6-deoxy-L-galactose, our strategy consists of the stereoselective construction of α-L-galactoside and its conversion to α-L-fucoside via C6-deoxygenation. In this study, the usefulness of fluorous chemistry has been examined for the practical construction of polysaccharide molecules like fucoidan and it was found that FSPE (Fluorous Solid Phase Extraction) was useful for quick purification of the desired product. Methods established in this study delivered alpha(1,3)-L-fucosyl oligomer (fucan) in good yields. Finally, sulfonation of hydroxyl groups in fucan furnished structurally-defined fucoidan molecule.
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| Academic Significance and Societal Importance of the Research Achievements |
従前、フコイダンの生理機能に関する研究は、天然の海草類から抽出した言わば混じり物で行われてきたため、フコイダンの分子構造と生理活性の関係性が真に評価されていなかった。そこで本研究では、有機化学的アプローチにより構造明確で純粋なフコイダン分子を創出することで、明瞭な構造活性相関のデータを取得し、フコイダンの多彩な生理活性を創薬などへ活かせると考えた。本研究では、独創的な化学合成法を開発し、それにより従来困難であった構造均一なフコイダン分子の創出に成功した。現在、合成した純粋なフコイダン分子を利用し、構造活性相関研究を進めている。
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Report
(4 results)
Research Products
(8 results)
