Activation of guinea pig peritoneal macrophages by platelet activating factor (PAF) and its agonists.
Activation of guinea pig peritoneal macrophages by platelet activating factor (PAF) and its agonists.
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血小板激活因子（PAF）及其激动剂对豚鼠腹腔巨噬细胞的激活。
DOI：
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发表时间：
1985
期刊：
影响因子：
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通讯作者：
S. Nojima
中科院分区：
文献类型：
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作者：
H. Hayashi;I. Kudo;K. Inoue;K. Onozaki;S. Tsushima;H. Nomura;S. Nojima
我们检测血小板活化因子（PAF: 1- o-烷基-2- o-乙酰- pn -甘油-3-磷酸胆碱）及其类似物对豚鼠腹腔巨噬细胞的影响。PAF激活巨噬细胞，但对巨噬细胞的作用远弱于对血小板的作用：50%最大激活所需浓度为巨噬细胞8.5 X 10(-6) M，血小板2.9 X 10(-10) M。三种PAF激动剂，1- o-十八烷基-2- o- （N，N-二甲基氨甲酰）-甘油-3-磷胆碱（化合物I）， 1- o-十八烷基-2-乙酰氨基-2-脱氧甘油-3-磷胆碱（化合物II）和1- o-十八烷基-2- o-甲基甘油-3-磷胆碱（化合物III），在刺激巨噬细胞功能方面表现出比PAF更高的活性。这些不可代谢的PAF激动剂激活巨噬细胞的能力与其诱导血小板激活的相对效力相似。PAF和化合物III的sn-3对映体具有活性，而sn-1对映体没有活性。通过比较化合物III衍生物的活性发现，甘油-1位的长链烷基醚基团、sn-2位羟基上相对小的取代基以及甘油-3位的胆碱基团在巨噬细胞活化过程中起着至关重要的作用。特异性PAF拮抗剂CV3988抑制PAF诱导的血小板活化和低血压，抑制PAF及其激动剂引起的巨噬细胞活化。（摘要删节250字）
The platelet activating factor (PAF: 1-O-alkyl-2-O-acetyl-sn-glycero-3-phosphocholine) and its analogs were examined to determine their effects on guinea pig peritoneal macrophages. PAF activated macrophages, but its effect on macrophages was much weaker than that observed on platelets: the concentration required for 50% maximum activation was 8.5 X 10(-6) M for macrophages and 2.9 X 10(-10) M for platelets. Three PAF agonists, 1-O-octadecyl-2-O-(N,N-dimethylcarbamoyl)-glycero-3-phosphocholine (Compound I), 1-O-octadecyl-2-acetamido-2-deoxy-glycero-3-phosphocholine (Compound II), and 1-O-octadecyl-2-O-methyl-glycero-3-phosphocholine (Compound III), showed higher activity in stimulating macrophage function than PAF. The abilities of these non-metabolizable PAF agonists to activate macrophage paralleled their relative potency to induce platelet activation. The sn-3 enantiomers of PAF and Compound III exhibited activity, while the sn-1 did not. By comparing the activities of derivatives of Compound III, it was shown that the long-chain alkyl-ether group in the glycerol-1 position, a relatively small size of the substituent on the hydroxy group at the sn-2 position, and the choline moiety in the glycerol-3 position must play critical roles in the process of macrophage activation. A specific PAF antagonist, CV3988, which inhibits PAF-induced platelet activation and hypotension, inhibited the activation of macrophages caused by PAF and its agonists.(ABSTRACT TRUNCATED AT 250 WORDS)