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Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent.
Br J Pharmacol 2015; 172(1):142-58BJ

Abstract

BACKGROUND AND PURPOSE

Palmitoylethanolamide (PEA) acts via several targets, including cannabinoid CB1 and CB2 receptors, transient receptor potential vanilloid type-1 (TRPV1) ion channels, peroxisome proliferator-activated receptor alpha (PPAR α) and orphan G protein-coupled receptor 55 (GRR55), all involved in the control of intestinal inflammation. Here, we investigated the effect of PEA in a murine model of colitis.

EXPERIMENTAL APPROACH

Colitis was induced in mice by intracolonic administration of dinitrobenzenesulfonic acid (DNBS). Inflammation was assessed by evaluating inflammatory markers/parameters and by histology; intestinal permeability by a fluorescent method; colonic cell proliferation by immunohistochemistry; PEA and endocannabinoid levels by liquid chromatography mass spectrometry; receptor and enzyme mRNA expression by quantitative RT-PCR.

KEY RESULTS

DNBS administration caused inflammatory damage, increased colonic levels of PEA and endocannabinoids, down-regulation of mRNA for TRPV1 and GPR55 but no changes in mRNA for CB1 , CB2 and PPARα. Exogenous PEA (i.p. and/or p.o., 1 mg·kg(-1)) attenuated inflammation and intestinal permeability, stimulated colonic cell proliferation, and increased colonic TRPV1 and CB1 receptor expression. The anti-inflammatory effect of PEA was attenuated or abolished by CB2 receptor, GPR55 or PPARα antagonists and further increased by the TRPV1 antagonist capsazepine.

CONCLUSIONS AND IMPLICATIONS

PEA improves murine experimental colitis, the effect being mediated by CB2 receptors, GPR55 and PPARα, and modulated by TRPV1 channels.

Authors+Show Affiliations

Department of Pharmacy, University of Naples Federico II, Naples, Italy.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

25205418

Citation

Borrelli, Francesca, et al. "Palmitoylethanolamide, a Naturally Occurring Lipid, Is an Orally Effective Intestinal Anti-inflammatory Agent." British Journal of Pharmacology, vol. 172, no. 1, 2015, pp. 142-58.
Borrelli F, Romano B, Petrosino S, et al. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent. Br J Pharmacol. 2015;172(1):142-58.
Borrelli, F., Romano, B., Petrosino, S., Pagano, E., Capasso, R., Coppola, D., ... Izzo, A. A. (2015). Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent. British Journal of Pharmacology, 172(1), pp. 142-58. doi:10.1111/bph.12907.
Borrelli F, et al. Palmitoylethanolamide, a Naturally Occurring Lipid, Is an Orally Effective Intestinal Anti-inflammatory Agent. Br J Pharmacol. 2015;172(1):142-58. PubMed PMID: 25205418.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent. AU - Borrelli,Francesca, AU - Romano,Barbara, AU - Petrosino,Stefania, AU - Pagano,Ester, AU - Capasso,Raffaele, AU - Coppola,Diana, AU - Battista,Giovanni, AU - Orlando,Pierangelo, AU - Di Marzo,Vincenzo, AU - Izzo,Angelo A, Y1 - 2014/12/01/ PY - 2013/12/11/received PY - 2014/08/01/revised PY - 2014/08/31/accepted PY - 2014/9/11/entrez PY - 2014/9/11/pubmed PY - 2015/9/5/medline SP - 142 EP - 58 JF - British journal of pharmacology JO - Br. J. Pharmacol. VL - 172 IS - 1 N2 - BACKGROUND AND PURPOSE: Palmitoylethanolamide (PEA) acts via several targets, including cannabinoid CB1 and CB2 receptors, transient receptor potential vanilloid type-1 (TRPV1) ion channels, peroxisome proliferator-activated receptor alpha (PPAR α) and orphan G protein-coupled receptor 55 (GRR55), all involved in the control of intestinal inflammation. Here, we investigated the effect of PEA in a murine model of colitis. EXPERIMENTAL APPROACH: Colitis was induced in mice by intracolonic administration of dinitrobenzenesulfonic acid (DNBS). Inflammation was assessed by evaluating inflammatory markers/parameters and by histology; intestinal permeability by a fluorescent method; colonic cell proliferation by immunohistochemistry; PEA and endocannabinoid levels by liquid chromatography mass spectrometry; receptor and enzyme mRNA expression by quantitative RT-PCR. KEY RESULTS: DNBS administration caused inflammatory damage, increased colonic levels of PEA and endocannabinoids, down-regulation of mRNA for TRPV1 and GPR55 but no changes in mRNA for CB1 , CB2 and PPARα. Exogenous PEA (i.p. and/or p.o., 1 mg·kg(-1)) attenuated inflammation and intestinal permeability, stimulated colonic cell proliferation, and increased colonic TRPV1 and CB1 receptor expression. The anti-inflammatory effect of PEA was attenuated or abolished by CB2 receptor, GPR55 or PPARα antagonists and further increased by the TRPV1 antagonist capsazepine. CONCLUSIONS AND IMPLICATIONS: PEA improves murine experimental colitis, the effect being mediated by CB2 receptors, GPR55 and PPARα, and modulated by TRPV1 channels. SN - 1476-5381 UR - https://www.unboundmedicine.com/medline/citation/25205418/Palmitoylethanolamide_a_naturally_occurring_lipid_is_an_orally_effective_intestinal_anti_inflammatory_agent_ L2 - https://doi.org/10.1111/bph.12907 DB - PRIME DP - Unbound Medicine ER -