Description
Prostaglandin E
2 ethanolamide (PGE
2-EA) is an analog of PGE
2 with improved water solubility and stability. PGE
2-EA is formed
via COX-2 metabolism of arachidonoyl ethanolamide (AEA; ) and acts as an agonist at E prostanoid (EP) receptors 1-4 (K
is = 2.45, 0.46, 0.2, and 0.51 μM, respectively). It also inhibits indoleamine 2,3-dioxygenase-1 (IDO-1) in THP-1 cells and human monocytes (IC
50s = 5.7 and 4.7 μM, respectively). PGE
2-EA (10 μM) prevents morphological changes and F-actin rearrangement as well as reduces L-homocysteine-induced NLRP3 inflammasome formation and activation in podocytes.
Ex vivo, PGE
2-EA reduces luminal damage and lymphocyte infiltration in a human mucosal explant colitis model.
Uses
Prostaglandin E2 Ethanolamide-d4 is the isotope labelled analogue of Prostaglandin E2 Ethanolamide, an analogue of Prostaglandin E2 (P838610). Prostaglandin E2 is most common and most biologically potent of mammalian prostaglandins.
References
[1] KEVIN R KOZAK. Metabolism of the endocannabinoids, 2-arachidonylglycerol and anandamide, into prostaglandin, thromboxane, and prostacyclin glycerol esters and ethanolamides.[J]. The Journal of Biological Chemistry, 2002, 277 47: 44877-44885. DOI:
10.1074/jbc.m206788200[2] TONG LIU. Intercellular transfer of the cellular prion protein.[J]. The Journal of Biological Chemistry, 2002, 277 49: 47671-47678. DOI:
10.1074/jbc.m207458200[3] M. COSTABILE . Inhibition of indoleamine 2,3-dioxygenase activity by fatty acids and prostaglandins: A structure function analysis[J]. Prostaglandins, leukotrienes, and essential fatty acids, 2017, 122: Pages 7-15. DOI:
10.1016/j.plefa.2017.06.010[4] GUANGBI LI. Protective Action of Anandamide and Its COX-2 Metabolite against l-Homocysteine-Induced NLRP3 Inflammasome Activation and Injury in Podocytes.[J]. Journal of Pharmacology and Experimental Therapeutics, 2016, 358 1: 61-70. DOI:
10.1124/jpet.116.233239[5] LAUREN L. NICOTRA. Prostaglandin ethanolamides attenuate damage in a human explant colitis model[J]. Prostaglandins & other lipid mediators, 2013, 100: Pages 22-29. DOI:
10.1016/j.prostaglandins.2013.01.003[6] ROBYN RICHIE-JANNETTA . Structural determinants for calcium mobilization by prostaglandin E2 and prostaglandin F2α glyceryl esters in RAW 264.7 cells and H1819 cells[J]. Prostaglandins & other lipid mediators, 2010, 92 1: Pages 19-24. DOI:
10.1016/j.prostaglandins.2010.01.003
