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

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...

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Autores principales: Arai, Midori A., Morita, Kaori, Kawano, Haruka, Makita, Yuna, Hashimoto, Manami, Suganami, Akiko, Tamura, Yutaka, Sadhu, Samir K., Ahmed, Firoj, Ishibashi, Masami
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6987128/
https://www.ncbi.nlm.nih.gov/pubmed/31992824
http://dx.doi.org/10.1038/s41598-020-58451-3
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author Arai, Midori A.
Morita, Kaori
Kawano, Haruka
Makita, Yuna
Hashimoto, Manami
Suganami, Akiko
Tamura, Yutaka
Sadhu, Samir K.
Ahmed, Firoj
Ishibashi, Masami
author_facet Arai, Midori A.
Morita, Kaori
Kawano, Haruka
Makita, Yuna
Hashimoto, Manami
Suganami, Akiko
Tamura, Yutaka
Sadhu, Samir K.
Ahmed, Firoj
Ishibashi, Masami
author_sort Arai, Midori A.
collection PubMed
description 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 IC(50) 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.
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spelling pubmed-69871282020-01-31 Target protein-oriented isolation of Hes1 dimer inhibitors using protein based methods Arai, Midori A. Morita, Kaori Kawano, Haruka Makita, Yuna Hashimoto, Manami Suganami, Akiko Tamura, Yutaka Sadhu, Samir K. Ahmed, Firoj Ishibashi, Masami Sci Rep Article 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 IC(50) 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. Nature Publishing Group UK 2020-01-28 /pmc/articles/PMC6987128/ /pubmed/31992824 http://dx.doi.org/10.1038/s41598-020-58451-3 Text en © The Author(s) 2020 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.
spellingShingle Article
Arai, Midori A.
Morita, Kaori
Kawano, Haruka
Makita, Yuna
Hashimoto, Manami
Suganami, Akiko
Tamura, Yutaka
Sadhu, Samir K.
Ahmed, Firoj
Ishibashi, Masami
Target protein-oriented isolation of Hes1 dimer inhibitors using protein based methods
title Target protein-oriented isolation of Hes1 dimer inhibitors using protein based methods
title_full Target protein-oriented isolation of Hes1 dimer inhibitors using protein based methods
title_fullStr Target protein-oriented isolation of Hes1 dimer inhibitors using protein based methods
title_full_unstemmed Target protein-oriented isolation of Hes1 dimer inhibitors using protein based methods
title_short Target protein-oriented isolation of Hes1 dimer inhibitors using protein based methods
title_sort target protein-oriented isolation of hes1 dimer inhibitors using protein based methods
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6987128/
https://www.ncbi.nlm.nih.gov/pubmed/31992824
http://dx.doi.org/10.1038/s41598-020-58451-3
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