論文

査読有り 国際誌
2020年1月28日

Target protein-oriented isolation of Hes1 dimer inhibitors using protein based methods.

Scientific reports
  • Midori A Arai
  • ,
  • Kaori Morita
  • ,
  • Haruka Kawano
  • ,
  • Yuna Makita
  • ,
  • Manami Hashimoto
  • ,
  • Akiko Suganami
  • ,
  • Yutaka Tamura
  • ,
  • Samir K Sadhu
  • ,
  • Firoj Ahmed
  • ,
  • Masami Ishibashi

10
1
開始ページ
1381
終了ページ
1381
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1038/s41598-020-58451-3

Natural products isolation using protein based methods is an attractive for obtaining bioactive compounds. To discover neural stem cell (NSC) differentiation activators, we isolated eight inhibitors of Hes1 dimer formation from Psidium guajava using the Hes1-Hes1 interaction fluorescent plate assay and one inhibitor from Terminalia chebula using the Hes1-immobilized beads method. Of the isolated compounds, gallic acid (8) and 4-O-(4"-O-galloyl-α-L-rhamnopyranosyl)ellagic acid (11) showed potent Hes1 dimer formation inhibitory activity, with IC50 values of 10.3 and 2.53 μM, respectively. Compound 11 accelerated the differentiation activity of C17.2 NSC cells dose dependently, increasing the number of neurons with a 125% increase (5 μM) compared to the control.

リンク情報
DOI
https://doi.org/10.1038/s41598-020-58451-3
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/31992824
PubMed Central
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6987128
ID情報
  • DOI : 10.1038/s41598-020-58451-3
  • PubMed ID : 31992824
  • PubMed Central 記事ID : PMC6987128

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