Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion
Abstract Objective Insulin secretion is regulated by ATP-sensitive potassium (KATP) 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,...
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| Format: | Article |
| Language: | English |
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BMC
2023-09-01
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| Series: | BMC Research Notes |
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| Online Access: | https://doi.org/10.1186/s13104-023-06489-7 |
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| author | Shigeki Kitamura Naoya Murao Shoko Yokota Masaru Shimizu Tomoyuki Ono Yusuke Seino Atsushi Suzuki Yuko Maejima Kenju Shimomura |
| author_facet | Shigeki Kitamura Naoya Murao Shoko Yokota Masaru Shimizu Tomoyuki Ono Yusuke Seino Atsushi Suzuki Yuko Maejima Kenju Shimomura |
| author_sort | Shigeki Kitamura |
| collection | DOAJ |
| description | Abstract Objective Insulin secretion is regulated by ATP-sensitive potassium (KATP) 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 KATP 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 KATP 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 KATP channel activity was measured by using whole-cell patch clamp technique. Although fenofibrate (100 µM) reduced the KATP channel current, the same concentration of pemafibrate had no effect. Both fenofibrate and pemafibrate had no effect on insulin mRNA expression. |
| first_indexed | 2024-03-10T22:20:58Z |
| format | Article |
| id | doaj.art-16b4b294cf154b6cb024b62b129c2711 |
| institution | Directory Open Access Journal |
| issn | 1756-0500 |
| language | English |
| last_indexed | 2024-03-10T22:20:58Z |
| publishDate | 2023-09-01 |
| publisher | BMC |
| record_format | Article |
| series | BMC Research Notes |
| spelling | doaj.art-16b4b294cf154b6cb024b62b129c27112023-11-19T12:16:26ZengBMCBMC Research Notes1756-05002023-09-011611810.1186/s13104-023-06489-7Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretionShigeki Kitamura0Naoya Murao1Shoko Yokota2Masaru Shimizu3Tomoyuki Ono4Yusuke Seino5Atsushi Suzuki6Yuko Maejima7Kenju Shimomura8Department of Bioregulation and Pharmacological Medicine, Fukushima Medical University School of MedicineDepartment of Endocrinology, Diabetes and Metabolism, Fujita Health UniversityDepartment of Bioregulation and Pharmacological Medicine, Fukushima Medical University School of MedicineDepartment of Bioregulation and Pharmacological Medicine, Fukushima Medical University School of MedicineDepartment of Bioregulation and Pharmacological Medicine, Fukushima Medical University School of MedicineDepartment of Endocrinology, Diabetes and Metabolism, Fujita Health UniversityDepartment of Endocrinology, Diabetes and Metabolism, Fujita Health UniversityDepartment of Bioregulation and Pharmacological Medicine, Fukushima Medical University School of MedicineDepartment of Bioregulation and Pharmacological Medicine, Fukushima Medical University School of MedicineAbstract Objective Insulin secretion is regulated by ATP-sensitive potassium (KATP) 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 KATP 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 KATP 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 KATP channel activity was measured by using whole-cell patch clamp technique. Although fenofibrate (100 µM) reduced the KATP channel current, the same concentration of pemafibrate had no effect. Both fenofibrate and pemafibrate had no effect on insulin mRNA expression.https://doi.org/10.1186/s13104-023-06489-7KATP channelPPARαfenofibratePemafibrate |
| spellingShingle | Shigeki Kitamura Naoya Murao Shoko Yokota Masaru Shimizu Tomoyuki Ono Yusuke Seino Atsushi Suzuki Yuko Maejima Kenju Shimomura Effect of fenofibrate and selective PPARα modulator (SPPARMα), pemafibrate on KATP channel activity and insulin secretion BMC Research Notes KATP channel PPARα fenofibrate Pemafibrate |
| 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 | KATP channel PPARα fenofibrate Pemafibrate |
| url | https://doi.org/10.1186/s13104-023-06489-7 |
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