Antidiabetic actions of an estrogen receptor β selective agonist

Paloma Alonso-Magdalena, Ana B. Ropero, Marta García-Arévalo, Sergi Soriano, Iván Quesada, Sarheed J. Muhammed, Albert Salehi, Jan Ake Gustafsson, Ángel Nadal

Research output: Contribution to journalArticle

36 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)2015-2025
Number of pages11
JournalDiabetes
Volume62
Issue number6
DOIs
StatePublished - Jun 2013

ASJC Scopus subject areas

  • Internal Medicine
  • Endocrinology, Diabetes and Metabolism

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