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The anti‐inflammatory mediator palmitoylethanolamide enhances the levels of 2‐arachidonoyl‐glycerol and potentiates its actions at TRPV1 cation channels

Petrosino, Stefania ; Schiano Moriello, Aniello ; Cerrato, Santiago ; Fusco, Mariella ; Puigdemont, Anna ; De Petrocellis, Luciano ; Di Marzo, Vincenzo

British journal of pharmacology, 2016-04, Vol.173 (7), p.1154-1162 [Periódico revisado por pares]

England: Blackwell Publishing Ltd

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The anti‐inflammatory mediator palmitoylethanolamide enhances the levels of 2‐arachidonoyl‐glycerol and potentiates its actions at TRPV1 cation channels
Autor: Petrosino, Stefania ; Schiano Moriello, Aniello ; Cerrato, Santiago ; Fusco, Mariella ; Puigdemont, Anna ; De Petrocellis, Luciano ; Di Marzo, Vincenzo
Assuntos: Adolescent ; Adult ; Amides ; Animals ; Anti-Inflammatory Agents, Non-Steroidal - pharmacology ; Arachidonic Acids - blood ; Calcium - metabolism ; Capsaicin - pharmacology ; Cell Line ; Dogs ; Endocannabinoids - blood ; Ethanolamines - metabolism ; Ethanolamines - pharmacology ; Female ; Glycerides - blood ; Humans ; Keratinocytes - drug effects ; Keratinocytes - metabolism ; Male ; Middle Aged ; Palmitic Acids - metabolism ; Palmitic Acids - pharmacology ; Research Paper ; Themed Section: Research Papers ; TRPV Cation Channels - agonists ; TRPV Cation Channels - metabolism ; Young Adult
É parte de: British journal of pharmacology, 2016-04, Vol.173 (7), p.1154-1162
Notas: ObjectType-Article-1
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These authors contributed equally to this work.
Descrição: Background and Purpose Palmitoylethanolamide (PEA) is an endogenous congener of anandamide and potentiates its actions at cannabinoid CB1 and CB2 receptors, and at transient receptor potential vanilloid type‐1 (TRPV1) channels. The other endocannabinoid, 2‐arachidonoylglycerol (2‐AG), was recently suggested to act as a TRPV1 channel agonist. We investigated if PEA enhanced levels of 2‐AG in vitro or in vivo and 2‐AG activity at TRPV1 channels. Experimental Approach Endogenous lipid levels were measured by LC‐MS in (i) human keratinocytes incubated with PEA (10–20 μM, 40 min, 6 and 24 h, 37°C); (ii) the blood of spontaneously Ascaris suum hypersensitive beagle dogs given a single oral dose of ultramicronized PEA (30 mg·kg−1, 1, 2, 4 and 8 h from administration); (iii) the blood of healthy volunteers given a single oral dose of micronized PEA (300 mg, 2, 4 and 6 h from administration). Effects of 2‐AG at TRPV1 channels were assessed by measuring intracellular Ca2+ in HEK‐293 cells over‐expressing human TRPV1 channels. Key Results PEA elevated 2‐AG levels in keratinocytes (∼3‐fold) and in human and canine plasma (∼2 and ∼20‐fold respectively). 2‐AG dose‐dependently raised intracellular Ca2+ in HEK‐293‐TRPV1 cells in a TRPV1‐dependent manner and desensitized the cells to capsaicin. PEA only slightly enhanced 2‐AG activation of TRPV1 channels, but significantly increased 2‐AG‐induced TRPV1 desensitization to capsaicin (IC50 from 0.75 ± 0.04 to 0.45 ± 0.02 μM, with PEA 2 μM). Conclusions and Implications These observations may explain why several effects of PEA are attenuated by cannabinoid receptor or TRPV1 channel antagonists. Linked Articles This article is part of a themed section on Endocannabinoids. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v173.7/issuetoc
Editor: England: Blackwell Publishing Ltd
Idioma: Inglês

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The anti‐inflammatory mediator palmitoylethanolamide enhances the levels of 2‐arachidonoyl‐glycerol and potentiates its actions at TRPV1 cation channels

Petrosino, Stefania ; Schiano Moriello, Aniello ; Cerrato, Santiago ; Fusco, Mariella ; Puigdemont, Anna ; De Petrocellis, Luciano ; Di Marzo, Vincenzo

England: Blackwell Publishing Ltd

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