Jambou D, Lapalus P
Department of Experimental and Clinical Pharmacology, Faculty of Medicine, University of Nice Sophia-Antipolis, France.
Int J Tissue React. 1990;12(5):273-80.
The magnesium salt of N acetyl-aspartyl glutamic acid (Naaga), used in ophthalmic allergies, is a synthetic dipeptide analogue of a natural peptide found in mammalian brains. It has been shown in vitro that Naaga inhibits complement activation, mast-cell degranulation and leukotriene anaphylactic release. In order to verify Naaga's action on leukotriene production, we used the macrophage cell line P388D1 activated by calcium ionophore A23187. Leukotriene determination was performed by high-performance liquid chromatography. It was found that Naaga inhibits 15 to 80% macrophage eicosanoid secretion (10(-9) M to 10(-2) M), acting mainly on LTC4-D4-E4 synthesis. Naaga was as potent as the leukotriene inhibitor nordihydroguaiaretic acid and as dexamethasone in this model. This inhibition of leukotriene secretion could partially explain the in-vivo antiallergic effects of Naaga.
N-乙酰天冬氨酰谷氨酸镁盐（Naaga）用于眼科过敏，是在哺乳动物大脑中发现的一种天然肽的合成二肽类似物。体外实验表明，Naaga可抑制补体激活、肥大细胞脱颗粒和白三烯过敏释放。为了验证Naaga对白三烯产生的作用，我们使用了由钙离子载体A23187激活的巨噬细胞系P388D1。通过高效液相色谱法测定白三烯。结果发现，Naaga抑制15%至80%的巨噬细胞类花生酸分泌（10⁻⁹ M至10⁻² M），主要作用于LTC4-D4-E4的合成。在该模型中，Naaga与白三烯抑制剂去甲二氢愈创木酸和地塞米松的效力相当。白三烯分泌的这种抑制作用可能部分解释了Naaga的体内抗过敏作用。
