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Capsaicin Analogues Derived from n-3 Polyunsaturated Fatty Acids (PUFAs) Reduce Inflammatory Activity of Macrophages and Stimulate Insulin Secretion by β-Cells In Vitro

1
Department of Pharmacy, Health and Nutritional Sciences, Department of Excellence 2018-2022, University of Calabria, 87036 Arcavacata di Rende (CS), Italy
2
Division of Human Nutrition and Health, Wageningen University, 6700 AA Wageningen, The Netherlands
*
Author to whom correspondence should be addressed.
Present address: Department of Diabetes, School of Life Course Sciences, King’s College London, London SE1 1UL, UK.
Nutrients 2019, 11(4), 915; https://doi.org/10.3390/nu11040915
Received: 22 March 2019 / Revised: 15 April 2019 / Accepted: 20 April 2019 / Published: 24 April 2019
(This article belongs to the Special Issue Nutrition and Insulin Resistance–Beyond Energy Metabolism)
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Abstract

In this study, two capsaicin analogues, N-eicosapentaenoyl vanillylamine (EPVA) and N-docosahexaenoyl vanillylamine (DHVA), were enzymatically synthesized from their corresponding n-3 long chain polyunsaturated fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), both dietary relevant components. The compounds significantly reduced the production of some lipopolysaccharide (LPS)-induced inflammatory mediators, including nitric oxide (NO), macrophage-inflammatory protein-3α (CCL20) and monocyte chemoattractant protein-1 (MCP-1 or CCL2), by RAW264.7 macrophages. Next to this, only EPVA increased insulin secretion by pancreatic INS-1 832/13 β-cells, while raising intracellular Ca2+ and ATP concentrations. This suggests that the stimulation of insulin release occurs through an increase in the intracellular ATP/ADP ratio in the first phase, while is calcium-mediated in the second phase. Although it is not yet known whether EPVA is endogenously produced, its potential therapeutic value for diabetes treatment merits further investigation. View Full-Text
Keywords: diabetes; fatty acid amides; inflammation; obesity; PUFA; vanillylamide diabetes; fatty acid amides; inflammation; obesity; PUFA; vanillylamide
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Cione, E.; Plastina, P.; Pingitore, A.; Perri, M.; Caroleo, M.C.; Fazio, A.; Witkamp, R.; Meijerink, J. Capsaicin Analogues Derived from n-3 Polyunsaturated Fatty Acids (PUFAs) Reduce Inflammatory Activity of Macrophages and Stimulate Insulin Secretion by β-Cells In Vitro. Nutrients 2019, 11, 915.

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