目的:观察糖皮质激素(GC)衍生物对巨噬细胞呼吸爆发的影响,并探讨GC对巨噬细胞呼吸爆发的非基因组作用机制。方法:合成亲水性和疏水性的系列GC衍生物,分离并培养腹腔巨噬细胞,应用细胞色素C还原法检测PMA刺激巨噬细胞生成超氧阴离子的能力。结果:获得了亲水性的GC衍生物氢化可的松-21-甘氨酸酯盐酸盐(HG)、氢化可的松-21-赖氨酸酯盐酸盐(HL)和疏水性的氢化可的松-21-苯丙氨酸酯盐酸盐(HP),HG和HL可显著促进PMA刺激巨噬细胞生成超氧阴离子,HP无显著作用。结论:GC快速增加PMA刺激的巨噬细胞超氧阴离子产生是通过非基因组机制实现的,这一作用与疏水性有关。
Objective: To observe the effects of glucocorticoid derivatives on respiratory burst in mouse peritoneal macrophages, and identify its nongenomic phenylalanine to get hydrophilic and hydrophobic glucocorticoid derivatives. Methods: Hydrocortisone conjugated with glycine, lysine and superoxide anions were measured by cytochrome C reduction assay to observe the effects on respiratory burst of mouse peritoneal macrophages. Results: Hydrophilic glucocorticoid derivatives, hydrocortisone-conjugated glycine (HG), hydrocortisone-conjugated lysine (HL), and hydrophobic hydrocortisone-conjugated phenylalanine (HP) were obtained. Hydrocortisone (HC), HG and HL could rapidly increase the superoxide anions production by macrophages, but HP did not. Conclusions: The effects of glucocorticoids on promoting the superoxide anions production by mouse peritoneal macrophages may be mediated by nongenomic mechanisms, which was related to hydro!ohobicity.