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

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

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Abstract

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.

Original languageEnglish
Article number1381
JournalScientific reports
Volume10
Issue number1
DOIs
Publication statusPublished - 2020 Dec 1

ASJC Scopus subject areas

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    Arai, M. A., Morita, K., Kawano, H., Makita, Y., Hashimoto, M., Suganami, A., Tamura, Y., Sadhu, S. K., Ahmed, F., & Ishibashi, M. (2020). Target protein-oriented isolation of Hes1 dimer inhibitors using protein based methods. Scientific reports, 10(1), [1381]. https://doi.org/10.1038/s41598-020-58451-3