オメガ3脂肪酸などの迅速精密合成法の開発と 新しい抗炎症性脂肪酸の発見~ペプチドのように効率的・精密に多価不飽和脂肪酸を合成し、機能性脂肪酸を発見~

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2025-06-26 東京大学

東京大学の研究チームは、多価不飽和脂肪酸(オメガ3など)を固相合成法で迅速・精密に合成する世界初の技術を開発した。従来は数週間以上かかった合成が、数時間〜数日で可能となり、研究や創薬への応用が期待される。この手法により、新たな抗炎症性脂肪酸「Antiefin」を発見。細胞実験やマウス試験で高い効果を示した。本技術は、脂質創薬の発展や脂質の機能解明に貢献する革新的成果といえる。

オメガ3脂肪酸などの迅速精密合成法の開発と 新しい抗炎症性脂肪酸の発見~ペプチドのように効率的・精密に多価不飽和脂肪酸を合成し、機能性脂肪酸を発見~
多価不飽和脂肪酸の完全固相合成

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完全固相合成による多価不飽和脂肪酸および生体機能性類似体への迅速なアクセス Expedited access to polyunsaturated fatty acids and biofunctional analogues by full solid-phase synthesis

Yutaro Saito,Mayuko Akita,Azusa Saika,Yusuke Sano,Masashi Hotta,Jumpei Morimoto,Akiharu Uwamizu,Junken Aoki,Takahiro Nagatake,Jun Kunisawa & Shinsuke Sando
Nature Chemistry  Published:25 June 2025
DOI:https://doi.org/10.1038/s41557-025-01853-5

Abstract

Polyunsaturated fatty acids (PUFAs) represent a fundamental and essential class of lipids that exhibit versatile biofunctions. Lipidomic analysis has identified a growing number of lipid species, including PUFAs with diverse structural variations and biofunctions, yet their structure–function relationships are still largely unknown. In this context, an efficient synthesis of PUFAs would be highly desirable. However, no practical methodology exists for their preparation, in contrast to peptides and nucleic acids, for which diverse molecules are accessible through a well-established solid-phase synthesis. To address this, we have developed an efficient and expedited method to access a wide array of PUFAs by full solid-phase synthesis. The method allows the synthesis of various PUFAs and analogues through rapid and facile operations. Moreover, within our PUFA library, we have discovered an artificial fatty acid, antiefin, that has a high anti-inflammatory effect in vivo. Therefore, our practical synthetic pathway to PUFAs, a crucial class of lipids, is expected to make an important contribution to lipid science.

有機化学・薬学
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