Fan T P, Lewis G P
Prostaglandins. 1985 Nov;30(5):735-47. doi: 10.1016/0090-6980(85)90004-8.
In vitro studies of PG production over a 24 h period by adherent rat peritoneal macrophages activated by serum-opsonized zymosan revealed that CSA (0.3-10 micrograms/ml) caused a dose-related inhibition of PGI2 (assayed as 6-oxo-PGF1 alpha) formation. Indomethacin (IND, 0.01-10 micrograms/ml) and dexamethasone (DEX, 0.01-10 micrograms/ml) also inhibited the PG production in a dose-related manner. When arachidonic acid (10 micrograms/ml) was added together with the inhibitors, there was no change in the level of PGI2 produced by IND-treated cells whilst the PGI2 levels of DEX- and CSA-treated cells were elevated to the control level. Therefore CSA like DEX does not inhibit cyclo-oxygenase activity. However unlike DEX, CSA (1-30 micrograms/ml) caused inhibition of phospholipase A2 (PLA2) activity when assayed on the hydrolysis of a synthetic substrate by pancreatic PLA2 in a cell-free system. The direct inhibition of PLA2 might well be a manifestation of the fundamental activity of CSA on immunocompetent cells.
通过血清调理酵母聚糖激活的贴壁大鼠腹膜巨噬细胞在24小时内产生前列腺素（PG）的体外研究表明，环孢素A（CSA，0.3 - 10微克/毫升）对前列环素（PGI2，以6 - 氧代 - PGF1α测定）的形成呈剂量相关的抑制作用。吲哚美辛（IND，0.01 - 10微克/毫升）和地塞米松（DEX，0.01 - 10微克/毫升）也以剂量相关的方式抑制PG的产生。当与抑制剂一起加入花生四烯酸（10微克/毫升）时，IND处理的细胞产生的PGI2水平没有变化，而DEX和CSA处理的细胞的PGI2水平升高到对照水平。因此，CSA与DEX一样不抑制环氧化酶活性。然而，与DEX不同的是，在无细胞系统中，当通过胰腺磷脂酶A2（PLA2）对合成底物的水解进行测定时，CSA（1 - 30微克/毫升）会抑制磷脂酶A2（PLA2）的活性。PLA2的直接抑制很可能是CSA对免疫活性细胞基本作用的一种表现。
