Cox C C, Dougherty R W, Ganong B R, Bell R M, Niedel J E, Snyderman R
J Immunol. 1986 Jun 15;136(12):4611-6.
Binding of chemoattractants to receptors on human polymorphonuclear leukocytes (PMN) stimulates the phosphodiesteric cleavage of phosphatidylinositol 4,5-bisphosphate to produce inositol 1,4,5-trisphosphate and 1,2-diacylglycerols. To investigate the possible second messenger function of diacylglycerols in PMN activation, we tested the ability of a series of synthetic sn 1,2-diacylglycerols, known to stimulate protein kinase C in other systems, to promote superoxide anion release, oxygen consumption, lysosomal enzyme secretion, and chemotaxis. None of the diacylglycerols initiated the chemotactic migration of PMN. Several of the diacylglycerols however, were, active in stimulating superoxide anion release and lysozyme secretion, with dioctanoylglycerol (diC8) being the most potent. Unexpectedly, didecanoylglycerol (diC10) induced lysosomal enzyme secretion, but failed to stimulate superoxide production or oxygen consumption. All other biologically active diacylglycerols tested displayed similar EC50 for stimulating lysozyme secretion and superoxide production. The ability of the diacylglycerols to compete for phorbol dibutyrate (PDBu) binding in intact PMN suggested a mechanism for the divergent biological activity of diC10. Although the compounds that stimulated both superoxide production and lysosomal enzyme secretion competed for essentially all [3H]PDBu binding from its receptor, diC10, which only stimulated secretion, competed for 45% of the bound [3H]PDBu. Thus diacylglycerols can selectively activate certain functions of leukocyte chemoattractant receptor. The data suggest that a discrete pool of protein kinase C may mediate activation of the respiratory burst in PMN.
趋化因子与人类多形核白细胞(PMN)上的受体结合,刺激磷脂酰肌醇4,5 - 二磷酸的磷酸二酯键裂解,产生肌醇1,4,5 - 三磷酸和1,2 - 二酰基甘油。为了研究二酰基甘油在PMN激活中可能的第二信使功能,我们测试了一系列已知在其他系统中能刺激蛋白激酶C的合成sn 1,2 - 二酰基甘油促进超氧阴离子释放、耗氧量、溶酶体酶分泌和趋化作用的能力。没有一种二酰基甘油能引发PMN的趋化迁移。然而,几种二酰基甘油在刺激超氧阴离子释放和溶菌酶分泌方面具有活性,其中二辛酰甘油(diC8)最为有效。出乎意料的是,二癸酰甘油(diC10)诱导了溶酶体酶分泌,但未能刺激超氧产生或耗氧量。所有测试的其他生物活性二酰基甘油在刺激溶菌酶分泌和超氧产生方面显示出相似的半数有效浓度(EC50)。二酰基甘油在完整PMN中竞争佛波醇二丁酸酯(PDBu)结合的能力提示了diC10生物活性差异的机制。虽然刺激超氧产生和溶酶体酶分泌的化合物基本上能竞争其受体上所有的[3H]PDBu结合,但仅刺激分泌的diC10只能竞争45%的结合[3H]PDBu。因此,二酰基甘油可以选择性地激活白细胞趋化因子受体的某些功能。数据表明,蛋白激酶C的一个离散池可能介导PMN中呼吸爆发的激活。