Alhouayek Mireille, Masquelier Julien, Muccioli Giulio G
Bioanalysis and Pharmacology of Bioactive Lipids Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 72, B1.72.01, B-1200 Bruxelles, Belgium; Medicinal Chemistry Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 73, B1.73.10, B-1200 Bruxelles, Belgium.
Bioanalysis and Pharmacology of Bioactive Lipids Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 72, B1.72.01, B-1200 Bruxelles, Belgium.
Drug Discov Today. 2014 Mar;19(3):295-304. doi: 10.1016/j.drudis.2013.07.009. Epub 2013 Jul 23.
The endocannabinoid system is implicated in, and regulates, several physiological processes, ranging from food intake and energy balance to pain and inflammation. 2-Arachidonoylglycerol (2-AG) is a full agonist at the cannabinoid receptors which classically mediate its effects. The activity of this bioactive lipid is dependent on its endogenous levels, which are tightly controlled by several hydrolases, monoacylglycerol lipase and α/β-hydrolase domain 6 and 12. Moreover, 2-AG is also a substrate of cyclooxygenase-2, and this reaction leads to the formation of prostaglandin glycerol esters, the effects of which remain to be fully elucidated. In this review we discuss the multiple mechanisms by which 2-AG controls inflammation and the therapeutic potential of 2-AG metabolism inhibitors.
内源性大麻素系统参与并调节多种生理过程，从食物摄入、能量平衡到疼痛和炎症。2-花生四烯酸甘油酯（2-AG）是大麻素受体的完全激动剂，经典地介导其效应。这种生物活性脂质的活性取决于其内源水平，而内源水平受到几种水解酶、单酰基甘油脂肪酶以及α/β水解酶结构域6和12的严格控制。此外，2-AG也是环氧化酶-2的底物，该反应导致前列腺素甘油酯的形成，其作用仍有待充分阐明。在本综述中，我们讨论了2-AG控制炎症的多种机制以及2-AG代谢抑制剂的治疗潜力。
