2011年12月
5-Hydroxy-eicosapentaenoic acid is an endogenous GPR119 agonist and enhances glucose-dependent insulin secretion
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
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- 巻
- 416
- 号
- 1-2
- 開始ページ
- 58
- 終了ページ
- 63
- 記述言語
- 英語
- 掲載種別
- DOI
- 10.1016/j.bbrc.2011.10.141
- 出版者・発行元
- ACADEMIC PRESS INC ELSEVIER SCIENCE
GPR119 is one of the G-protein-coupled receptors expressed in pancreatic beta-cells and intestinal endocrine cells. Since agonists to GPR119 stimulate glucose-dependent insulin secretion. GPR119 agonists are anticipated to promote anti-diabetic effects and control of glucose homeostasis. Here, we reported that an omega-3 unsaturated fatty acid metabolite, 5-hydroxy-eicosapentaenoic acid (5-HEPE), was a potent agonist for GPR119 and enhanced glucose-dependent insulin secretion. 5-HEPE stimulated cAMP accumulation in mouse MIN6 insulinoma cells and human HuTu80 intestinal adenocarcinoma cells. These effects were blunted by GPR119-specific siRNA. Recombinant GPR119 also responded to 5-HEPE as well as authentic agonists. Several previous reports have indicated the beneficial biological effects of omega-3 unsaturated fatty acids, and epidemiological studies have suggested that these fatty acids plays a protective role against diabetes. However, the molecular pharmacology and receptor identifications of omega-3 unsaturated fatty acids and their metabolites have not yet been well investigated. It is hoped that our findings will encourage novel investigations into the molecular relationships between omega-3 fatty acids and diabetes. (C) 2011 Elsevier Inc. All rights reserved.
- リンク情報
- ID情報
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- DOI : 10.1016/j.bbrc.2011.10.141
- ISSN : 0006-291X
- Web of Science ID : WOS:000298222100010