|Title||Capsaicin analogues derived from n-3 polyunsaturated fatty acids (PUFAs) reduce inflammatory activity of macrophages and stimulate insulin secretion by β-cells in vitro|
|Author(s)||Cione, Erika; Plastina, Pierluigi; Pingitore, Attilio; Perri, Mariarita; Caroleo, Maria Cristina; Fazio, Alessia; Witkamp, Renger; Meijerink, Jocelijn|
|Source||Nutrients 11 (2019)4. - ISSN 2072-6643|
Nutritional Biology and Health
|Publication type||Refereed Article in a scientific journal|
|Keyword(s)||Diabetes - Fatty acid amides - Inflammation - Obesity - PUFA - Vanillylamide|
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 Ca 2+ 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.