非甾体抗炎药对高度纯化的哺乳动物磷脂酶A2的抑制作用。钙离子的调节作用。
Inhibition of highly purified mammalian phospholipases A2 by non-steroidal anti-inflammatory agents. Modulation by calcium ions.
作者信息
Franson R C, Eisen D, Jesse R, Lanni C
出版信息
Biochem J. 1980 Feb 15;186(2):633-6. doi: 10.1042/bj1860633.
Abstract
Highly purified Ca2+-dependent phospholipases A2 that were isolated from human platelets, rabbit alveolar macrophages and peritoneal polymorphonuclear leucocytes and were active in the neutral-to-alkaline pH range were inhibited 50% by 75 microM-indomethacin in the presence of 5.0 mM added Ca2+. Sodium meclofenamate and sodium flufenamate were also inhibitory; the sensitivity to inhibition was a function of Ca2+ concentration. The dose for 50% inhibition (ID50) with meclofenamate was 0.4 mM in the presence of 2.5 mM added Ca2+, but 50nM in the presence of 0.5 mM added Ca2+. Thus, inhibition of phospholipase A2 activity by non-steroidal anti-inflammatory agents via Ca2+ antagonism may significantly contribute to the mechanism of drug action.
摘要
从人血小板、兔肺泡巨噬细胞和腹膜多形核白细胞中分离出的高度纯化的钙依赖性磷脂酶A2，在中性至碱性pH范围内具有活性，在添加5.0 mM Ca2+的情况下，75 microM消炎痛可抑制其活性50%。甲氯芬那酸钠和氟芬那酸钠也具有抑制作用；对抑制的敏感性是Ca2+浓度的函数。在添加2.5 mM Ca2+的情况下，甲氯芬那酸50%抑制剂量（ID50）为0.4 mM，但在添加0.5 mM Ca2+的情况下为50 nM。因此，非甾体抗炎药通过Ca2+拮抗作用抑制磷脂酶A2活性可能对药物作用机制有显著贡献。
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