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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)
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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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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