天然有機化合物討論会講演要旨集
Online ISSN : 2433-1856
第59回天然有機化合物討論会実行委員会
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23 標的タンパク質指向型天然物単離による生物活性天然物の探索 (口頭発表の部)
*荒井 緑越智 富美江林 奈留美橋本 真波田中 光葉田内 伽奈石川 直樹Ahmed FirojSadhu Samir K.石橋 正己
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会議録・要旨集 オープンアクセス

p. 133-138

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Binding affinity to protein is one of the important property for biological activity. Recently, we have developed “Target protein oriented natural products isolation (TPO-NAPI)” method to isolation of bioactive natural products. Protein immobilized sepharose beads were prepared and mixed with extract of natural resources. After incubation and wash process, bound compounds were released from protein beads by addition EtOH. Hairy and enhancer of split 1 (Hes1) is a repressor type basic helix-loop-helix factor which inhibits neural stem cells (NSCs) differentiation. Hes1 beads gave two new compounds 1, 2 which accelerated NSCs differentiation. Notch intracellular domain (NICD) is a transcriptional factor in Notch signal pathway. Aciculatin 5 was found as a Notch inhibitor by NICD beads method. Compound 5 also enhanced the differentiation of NSCs. Hedgehog (Hh) signal is one of the central signals in cell maintenance and differentiation. GLI1, a transcriptional factor in Hh signal, was immobilized on beads, which gave five natural products 9-13. This TPO-NAPI method would be useful to isolate target protein binding natural products from extract of natural resources.

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