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Antidiabetic Actions of an Estrogen Receptor β Selective Agonist
The estrogen receptor β (ERβ) is emerging as an important player in the physiology of the endocrine pancreas. We evaluated the role and antidiabetic actions of the ERβ selective agonist WAY200070 as an insulinotropic molecule. We demonstrate that WAY200070 enhances glucose-stimulated insulin secreti...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Diabetes Association
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3661616/ https://www.ncbi.nlm.nih.gov/pubmed/23349481 http://dx.doi.org/10.2337/db12-1562 |
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author | Alonso-Magdalena, Paloma Ropero, Ana B. García-Arévalo, Marta Soriano, Sergi Quesada, Iván Muhammed, Sarheed J. Salehi, Albert Gustafsson, Jan-Ake Nadal, Ángel |
author_facet | Alonso-Magdalena, Paloma Ropero, Ana B. García-Arévalo, Marta Soriano, Sergi Quesada, Iván Muhammed, Sarheed J. Salehi, Albert Gustafsson, Jan-Ake Nadal, Ángel |
author_sort | Alonso-Magdalena, Paloma |
collection | PubMed |
description | The estrogen receptor β (ERβ) is emerging as an important player in the physiology of the endocrine pancreas. We evaluated the role and antidiabetic actions of the ERβ selective agonist WAY200070 as an insulinotropic molecule. We demonstrate that WAY200070 enhances glucose-stimulated insulin secretion both in mouse and human islets. In vivo experiments showed that a single administration of WAY200070 leads to an increase in plasma insulin levels with a concomitant improved response to a glucose load. Two-week treatment administration increased glucose-induced insulin release and pancreatic β-cell mass and improved glucose and insulin sensitivity. In addition, streptozotocin-nicotinamide–induced diabetic mice treated with WAY200070 exhibited a significant improvement in plasma insulin levels and glucose tolerance as well as a regeneration of pancreatic β-cell mass. Studies performed in db/db mice demonstrated that this compound restored first-phase insulin secretion and enhanced pancreatic β-cell mass. We conclude that ERβ agonists should be considered as new targets for the treatment of diabetes. |
format | Online Article Text |
id | pubmed-3661616 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | American Diabetes Association |
record_format | MEDLINE/PubMed |
spelling | pubmed-36616162014-06-01 Antidiabetic Actions of an Estrogen Receptor β Selective Agonist Alonso-Magdalena, Paloma Ropero, Ana B. García-Arévalo, Marta Soriano, Sergi Quesada, Iván Muhammed, Sarheed J. Salehi, Albert Gustafsson, Jan-Ake Nadal, Ángel Diabetes Original Research The estrogen receptor β (ERβ) is emerging as an important player in the physiology of the endocrine pancreas. We evaluated the role and antidiabetic actions of the ERβ selective agonist WAY200070 as an insulinotropic molecule. We demonstrate that WAY200070 enhances glucose-stimulated insulin secretion both in mouse and human islets. In vivo experiments showed that a single administration of WAY200070 leads to an increase in plasma insulin levels with a concomitant improved response to a glucose load. Two-week treatment administration increased glucose-induced insulin release and pancreatic β-cell mass and improved glucose and insulin sensitivity. In addition, streptozotocin-nicotinamide–induced diabetic mice treated with WAY200070 exhibited a significant improvement in plasma insulin levels and glucose tolerance as well as a regeneration of pancreatic β-cell mass. Studies performed in db/db mice demonstrated that this compound restored first-phase insulin secretion and enhanced pancreatic β-cell mass. We conclude that ERβ agonists should be considered as new targets for the treatment of diabetes. American Diabetes Association 2013-06 2013-05-17 /pmc/articles/PMC3661616/ /pubmed/23349481 http://dx.doi.org/10.2337/db12-1562 Text en © 2013 by the American Diabetes Association. Readers may use this article as long as the work is properly cited, the use is educational and not for profit, and the work is not altered. See http://creativecommons.org/licenses/by-nc-nd/3.0/ for details. |
spellingShingle | Original Research Alonso-Magdalena, Paloma Ropero, Ana B. García-Arévalo, Marta Soriano, Sergi Quesada, Iván Muhammed, Sarheed J. Salehi, Albert Gustafsson, Jan-Ake Nadal, Ángel Antidiabetic Actions of an Estrogen Receptor β Selective Agonist |
title | Antidiabetic Actions of an Estrogen Receptor β Selective Agonist |
title_full | Antidiabetic Actions of an Estrogen Receptor β Selective Agonist |
title_fullStr | Antidiabetic Actions of an Estrogen Receptor β Selective Agonist |
title_full_unstemmed | Antidiabetic Actions of an Estrogen Receptor β Selective Agonist |
title_short | Antidiabetic Actions of an Estrogen Receptor β Selective Agonist |
title_sort | antidiabetic actions of an estrogen receptor β selective agonist |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3661616/ https://www.ncbi.nlm.nih.gov/pubmed/23349481 http://dx.doi.org/10.2337/db12-1562 |
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