Camp R D, Fincham N J
Br J Pharmacol. 1985 Aug;85(4):837-41. doi: 10.1111/j.1476-5381.1985.tb11082.x.
Leukotriene B4 (LTB4) release by calcium ionophore-stimulated human leucocytes was measured by use of selective solvent partition of reaction mixtures and an agarose microdroplet chemokinesis assay, and the inhibitory effects of four monohydroxy fatty acids were determined. 15-Hydroxy-eicosatetraenoic acid (15-HETE) was the most effective inhibitor of LTB4 production with an approximate IC50 value of 6 microM and 99% inhibition at 50 microM, whereas 13-hydroxy-octadecadienoic acid (13-HODD) and 12-HETE were weaker inhibitors with approximate IC50 values of 32 microM and 23 microM, and 59% and 68% inhibition at 50 microM, respectively. We suggest that 13-HODD and 12-HETE, which are present in large amounts in the lesions of the skin disease psoriasis, may act as endogenous modulators of 5-lipoxygenase activity in skin.
通过对反应混合物进行选择性溶剂分配以及使用琼脂糖微滴趋化性测定法,来测量钙离子载体刺激的人白细胞释放白三烯B4(LTB4)的情况,并确定了四种单羟基脂肪酸的抑制作用。15-羟基-二十碳四烯酸(15-HETE)是LTB4生成的最有效抑制剂,其近似IC50值为6微摩尔,在50微摩尔时抑制率达99%,而13-羟基-十八碳二烯酸(13-HODD)和12-HETE是较弱的抑制剂,近似IC50值分别为32微摩尔和23微摩尔,在50微摩尔时抑制率分别为59%和68%。我们认为,在皮肤病牛皮癣的皮损中大量存在的13-HODD和12-HETE,可能作为皮肤中5-脂氧合酶活性的内源性调节剂。