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Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion

OBJECTIVE: Insulin secretion is regulated by ATP-sensitive potassium (K(ATP)) channels in pancreatic beta-cells. Peroxisome proliferator-activated receptors (PPAR) α ligands are clinically used to treat dyslipidemia. A PPARα ligand, fenofibrate, and PPARγ ligands troglitazone and 15-deoxy-∆(12,14)-p...

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Autores principales: Kitamura, Shigeki, Murao, Naoya, Yokota, Shoko, Shimizu, Masaru, Ono, Tomoyuki, Seino, Yusuke, Suzuki, Atsushi, Maejima, Yuko, Shimomura, Kenju
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10494450/
https://www.ncbi.nlm.nih.gov/pubmed/37697384
http://dx.doi.org/10.1186/s13104-023-06489-7
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author Kitamura, Shigeki
Murao, Naoya
Yokota, Shoko
Shimizu, Masaru
Ono, Tomoyuki
Seino, Yusuke
Suzuki, Atsushi
Maejima, Yuko
Shimomura, Kenju
author_facet Kitamura, Shigeki
Murao, Naoya
Yokota, Shoko
Shimizu, Masaru
Ono, Tomoyuki
Seino, Yusuke
Suzuki, Atsushi
Maejima, Yuko
Shimomura, Kenju
author_sort Kitamura, Shigeki
collection PubMed
description OBJECTIVE: Insulin secretion is regulated by ATP-sensitive potassium (K(ATP)) channels in pancreatic beta-cells. Peroxisome proliferator-activated receptors (PPAR) α ligands are clinically used to treat dyslipidemia. A PPARα ligand, fenofibrate, and PPARγ ligands troglitazone and 15-deoxy-∆(12,14)-prostaglandin J2 are known to close K(ATP) channels and induce insulin secretion. The recently developed PPARα ligand, pemafibrate, became a new entry for treating dyslipidemia. Because pemafibrate is reported to improve glucose intolerance in mice treated with a high fat diet and a novel selective PPARα modulator, it may affect K(ATP) channels or insulin secretion. RESULTS: The effect of fenofibrate (100 µM) and pemafibrate (100 µM) on insulin secretion from MIN6 cells was measured by using batch incubation for 10 and 60 min in low (2 mM) and high (10 mM) glucose conditions. The application of fenofibrate for 10 min significantly increased insulin secretion in low glucose conditions. Pemafibrate failed to increase insulin secretion in all of the conditions experimented in this study. The K(ATP) channel activity was measured by using whole-cell patch clamp technique. Although fenofibrate (100 µM) reduced the K(ATP) channel current, the same concentration of pemafibrate had no effect. Both fenofibrate and pemafibrate had no effect on insulin mRNA expression.
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spelling pubmed-104944502023-09-12 Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion Kitamura, Shigeki Murao, Naoya Yokota, Shoko Shimizu, Masaru Ono, Tomoyuki Seino, Yusuke Suzuki, Atsushi Maejima, Yuko Shimomura, Kenju BMC Res Notes Research Note OBJECTIVE: Insulin secretion is regulated by ATP-sensitive potassium (K(ATP)) channels in pancreatic beta-cells. Peroxisome proliferator-activated receptors (PPAR) α ligands are clinically used to treat dyslipidemia. A PPARα ligand, fenofibrate, and PPARγ ligands troglitazone and 15-deoxy-∆(12,14)-prostaglandin J2 are known to close K(ATP) channels and induce insulin secretion. The recently developed PPARα ligand, pemafibrate, became a new entry for treating dyslipidemia. Because pemafibrate is reported to improve glucose intolerance in mice treated with a high fat diet and a novel selective PPARα modulator, it may affect K(ATP) channels or insulin secretion. RESULTS: The effect of fenofibrate (100 µM) and pemafibrate (100 µM) on insulin secretion from MIN6 cells was measured by using batch incubation for 10 and 60 min in low (2 mM) and high (10 mM) glucose conditions. The application of fenofibrate for 10 min significantly increased insulin secretion in low glucose conditions. Pemafibrate failed to increase insulin secretion in all of the conditions experimented in this study. The K(ATP) channel activity was measured by using whole-cell patch clamp technique. Although fenofibrate (100 µM) reduced the K(ATP) channel current, the same concentration of pemafibrate had no effect. Both fenofibrate and pemafibrate had no effect on insulin mRNA expression. BioMed Central 2023-09-11 /pmc/articles/PMC10494450/ /pubmed/37697384 http://dx.doi.org/10.1186/s13104-023-06489-7 Text en © The Author(s) 2023 https://creativecommons.org/licenses/by/4.0/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 licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence 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 licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) . The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/ (https://creativecommons.org/publicdomain/zero/1.0/) ) applies to the data made available in this article, unless otherwise stated in a credit line to the data.
spellingShingle Research Note
Kitamura, Shigeki
Murao, Naoya
Yokota, Shoko
Shimizu, Masaru
Ono, Tomoyuki
Seino, Yusuke
Suzuki, Atsushi
Maejima, Yuko
Shimomura, Kenju
Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion
title Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion
title_full Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion
title_fullStr Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion
title_full_unstemmed Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion
title_short Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion
title_sort effect of fenofibrate and selective pparα modulator (spparmα), pemafibrate on katp channel activity and insulin secretion
topic Research Note
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10494450/
https://www.ncbi.nlm.nih.gov/pubmed/37697384
http://dx.doi.org/10.1186/s13104-023-06489-7
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