Olive Oil Lipophenols Induce Insulin Secretion in 832/13 β-Cell Models
Glycemic control is a mainstay of type 2 diabetes mellitus (T2DM) clinical management. Despite the continuous improvement in knowledge and progress in terms of treatment, the achievement of the physiologic metabolic profile is still an ongoing challenge in diabetic patients. Pancreatic β-cell line I...
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| Format: | Article |
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MDPI AG
2021-07-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/7/1085 |
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| author | Maria Cristina Caroleo Pierluigi Plastina Alessia Fazio Chiara La Torre Fabrizio Manetti Erika Cione |
| author_facet | Maria Cristina Caroleo Pierluigi Plastina Alessia Fazio Chiara La Torre Fabrizio Manetti Erika Cione |
| author_sort | Maria Cristina Caroleo |
| collection | DOAJ |
| description | Glycemic control is a mainstay of type 2 diabetes mellitus (T2DM) clinical management. Despite the continuous improvement in knowledge and progress in terms of treatment, the achievement of the physiologic metabolic profile is still an ongoing challenge in diabetic patients. Pancreatic β-cell line INS-1 832/13 was used to assess the insulin secretagogue activity of hydroxytyrosyl oleate (HtyOle) and tyrosyl oleate (TyOle), two naturally occurring lipophenols deriving from the conjugation of oleic acid (OA) and hydroxytyrosol (Hty) or tyrosol (Ty), respectively. The insulin secretion was determined under a glucose-induced insulin secretion (GSIS) condition by the ELISA method. The potential involvement of G-protein-coupled receptor 40 (GPR40), also known as free fatty acid receptor 1 (FFAR1), was investigated by both molecular docking and functional pharmacological approaches. Herein, we demonstrated that HtyOle and TyOle exerted a facilitatory activity on insulin secretion under the GSIS condition. Moreover, we provided evidence that both lipophenols are natural modulators of FFAR1 receptor. From our results, the anti-diabetes properties associated with olive oil consumption can be partly explained by the HtyOle and TyOle effects. |
| first_indexed | 2024-03-10T09:28:09Z |
| format | Article |
| id | doaj.art-05463b2dc49f4ab5a3152fd90a2d4886 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T09:28:09Z |
| publishDate | 2021-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-05463b2dc49f4ab5a3152fd90a2d48862023-11-22T04:41:52ZengMDPI AGPharmaceutics1999-49232021-07-01137108510.3390/pharmaceutics13071085Olive Oil Lipophenols Induce Insulin Secretion in 832/13 β-Cell ModelsMaria Cristina Caroleo0Pierluigi Plastina1Alessia Fazio2Chiara La Torre3Fabrizio Manetti4Erika Cione5Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyDepartment of Biotechnology, Chemistry and Pharmacy, University of Siena, Via Aldo Moro 2, I-53100 Siena, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, ItalyGlycemic control is a mainstay of type 2 diabetes mellitus (T2DM) clinical management. Despite the continuous improvement in knowledge and progress in terms of treatment, the achievement of the physiologic metabolic profile is still an ongoing challenge in diabetic patients. Pancreatic β-cell line INS-1 832/13 was used to assess the insulin secretagogue activity of hydroxytyrosyl oleate (HtyOle) and tyrosyl oleate (TyOle), two naturally occurring lipophenols deriving from the conjugation of oleic acid (OA) and hydroxytyrosol (Hty) or tyrosol (Ty), respectively. The insulin secretion was determined under a glucose-induced insulin secretion (GSIS) condition by the ELISA method. The potential involvement of G-protein-coupled receptor 40 (GPR40), also known as free fatty acid receptor 1 (FFAR1), was investigated by both molecular docking and functional pharmacological approaches. Herein, we demonstrated that HtyOle and TyOle exerted a facilitatory activity on insulin secretion under the GSIS condition. Moreover, we provided evidence that both lipophenols are natural modulators of FFAR1 receptor. From our results, the anti-diabetes properties associated with olive oil consumption can be partly explained by the HtyOle and TyOle effects.https://www.mdpi.com/1999-4923/13/7/1085lipophenolsFFAR1GSISinsulin secretionhydroxytyrosoltyrosol |
| spellingShingle | Maria Cristina Caroleo Pierluigi Plastina Alessia Fazio Chiara La Torre Fabrizio Manetti Erika Cione Olive Oil Lipophenols Induce Insulin Secretion in 832/13 β-Cell Models Pharmaceutics lipophenols FFAR1 GSIS insulin secretion hydroxytyrosol tyrosol |
| title | Olive Oil Lipophenols Induce Insulin Secretion in 832/13 β-Cell Models |
| title_full | Olive Oil Lipophenols Induce Insulin Secretion in 832/13 β-Cell Models |
| title_fullStr | Olive Oil Lipophenols Induce Insulin Secretion in 832/13 β-Cell Models |
| title_full_unstemmed | Olive Oil Lipophenols Induce Insulin Secretion in 832/13 β-Cell Models |
| title_short | Olive Oil Lipophenols Induce Insulin Secretion in 832/13 β-Cell Models |
| title_sort | olive oil lipophenols induce insulin secretion in 832 13 β cell models |
| topic | lipophenols FFAR1 GSIS insulin secretion hydroxytyrosol tyrosol |
| url | https://www.mdpi.com/1999-4923/13/7/1085 |
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