Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina (ME), Italy.
Department of Pharmacological and Physiological Science, Saint Louis University, Saint Louis, MO 63103, USA.
Int J Mol Sci. 2021 Feb 17;22(4):1967. doi: 10.3390/ijms22041967.
Palmitoylethanolamide (PEA), a fatty acid amide, has been widely investigated for its analgesic and anti-inflammatory properties. The ultra-micronized formulation of PEA (um-PEA), that has an enhanced rate of dissolution, is extensively used. Acetyl-l-carnitine (LAC), employed for the treatment of neuropathic pain in humans, is able to cause analgesia by up-regulating type-2 metabotropic glutamate (mGlu2) receptors. In the present study, we tested different associations of um-PEA, LAC and non-micronized PEA (non-m-PEA) in a rat model of carrageenan (CAR)-induced paw edema. Intraplantar injection of CAR into the hind paw of animals caused edema, thermal hyperalgesia, accumulation of infiltrating inflammatory cells and augmented myeloperoxidase (MPO) activity. All these parameters were decreased in a significantly manner by oral administration of a compound constituted by a mixture of um-PEA and LAC in relation 1:1 (5 mg/kg), but not with the association of single compounds administered one after the other. These findings showed the superior anti-inflammatory and anti-nociceptive action displayed by oral administration of um-PEA and LAC versus LAC plus, separate but consecutive, um-PEA in the rat paw CAR model of inflammatory pain.
棕榈酰乙醇酰胺(PEA),一种脂肪酸酰胺,因其具有镇痛和抗炎特性而被广泛研究。超微化 PEA 制剂(um-PEA)具有增强的溶解速率,被广泛应用。乙酰左旋肉碱(LAC)用于治疗人类的神经性疼痛,能够通过上调 2 型代谢型谷氨酸受体(mGlu2)来引起镇痛。在本研究中,我们在卡拉胶(CAR)诱导的爪肿胀大鼠模型中测试了 um-PEA、LAC 和非微化 PEA(非 m-PEA)的不同组合。将 CAR 注射到动物的后爪中会引起水肿、热痛觉过敏、浸润性炎症细胞的积累和髓过氧化物酶(MPO)活性的增加。所有这些参数均通过口服由 um-PEA 和 LAC 以 1:1(5mg/kg)的比例混合而成的化合物显著降低,但单独给予单一化合物的组合则没有这种效果。这些发现表明,与 LAC 加、单独但连续给予 um-PEA 相比,口服 um-PEA 和 LAC 对大鼠爪 CAR 炎症性疼痛模型显示出更好的抗炎和镇痛作用。