Zeng G Q, Rui Y C
Department of Pharmacology, College of Pharmacy, Second Military Medical University, Shanghai, China.
Zhongguo Yao Li Xue Bao. 1990 Jul;11(4):346-50.
The effects of dauricine (Dau) on the release of platelet activating factor (PAF) from mouse peritoneal macrophages stimulated by calcimycin (A-23187) was studied. The method of sodium [3H]acetate incorporating into macrophages to synthesize PAF was set up for the first time. Calcimycin (0.2 mumol/L) significantly induced mouse peritoneal macrophages to utilize sodium [3H]acetate to synthesize PAF. PAF released from macrophages medium fluid increased as the concentration of sodium [3H]acetate increased. The maximal amount of PAF released from macrophages was attained by incubating macrophages with sodium [3H]acetate (250 mumol/L) and calcimycin (2 mumol/L) over 30 min. Extracted by CHCl3:CH3OH:H2O (2:2:1.8), separated by thin layer chromatography (TLC) and determined by liquid scintillation counting, PAF released was inhibited significantly by Dau both in time (10-30 min) and dose (1-1000 mumol/L) dependent manners. The IC50 of Dau for the formation of PAF was 2.5 mumol/L. On the same condition PAF release was also significantly inhibited by quinacrine at 500 mumol/L. The results indicate that Dau is a potent inhibitor of PAF synthesis in mouse peritoneal macrophages.
研究了蝙蝠葛碱(Dau)对离子霉素(A - 23187)刺激的小鼠腹腔巨噬细胞释放血小板活化因子(PAF)的影响。首次建立了用[³H]醋酸钠掺入巨噬细胞以合成PAF的方法。离子霉素(0.2 μmol/L)显著诱导小鼠腹腔巨噬细胞利用[³H]醋酸钠合成PAF。巨噬细胞培养液中释放的PAF随着[³H]醋酸钠浓度的增加而增加。用[³H]醋酸钠(250 μmol/L)和离子霉素(2 μmol/L)孵育巨噬细胞30分钟可达到从巨噬细胞释放PAF的最大量。通过氯仿:甲醇:水(2:2:1.8)萃取,薄层层析(TLC)分离并通过液体闪烁计数法测定,蝙蝠葛碱在时间(10 - 30分钟)和剂量(1 - 1000 μmol/L)依赖方式下均显著抑制PAF的释放。蝙蝠葛碱对PAF形成的IC50为2.5 μmol/L。在相同条件下,500 μmol/L的奎纳克林也显著抑制PAF的释放。结果表明,蝙蝠葛碱是小鼠腹腔巨噬细胞中PAF合成的有效抑制剂。