Cholbi R, Ferrándiz M L, Terencio M C, De Rosa S, Alcaraz M J, Payá M
Department of Pharmacology, University of Valencia, Faculty of Pharmacy, Burjassot, Spain.
Naunyn Schmiedebergs Arch Pharmacol. 1996 Nov;354(5):677-83. doi: 10.1007/BF00170845.
The marine product ircinin has been tested for its effects on secretory and cytosolic phospholipase A2 (PLA2) activities in vitro as well as for inhibition of cellular functions in human neutrophils and inflammatory responses in mice. Ircinin inhibited Naja naja venom, human synovial recombinant, bee venom and zymosan-injected rat air pouch PLA2 with IC50 values in the microM range, similar to those of the known inhibitor scalaradial. On the other hand, ircinin was less active on cytosolic PLA2 from human monocytes and decreased potently the release of LTB4 in human neutrophils. This marine product affected weakly human neutrophil functions like superoxide generation and degranulation. In the zymosan-injected rat air pouch ircinin inhibited in vivo the activity of PLA2 present in exudates and reduced dose-dependently myeloperoxidase levels, whereas cell migration was inhibited only at the highest dose tested. This compound exerted a potent anti-oedematous effect after topical application in the mouse ear oedema test. Ircinin is a new inhibitor of PLA2 activity and our results suggest a potential role for this marine product as an inhibitor of inflammatory processes.
已对海产品ircinin在体外对分泌型和胞质型磷脂酶A2（PLA2）活性的影响以及对人中性粒细胞细胞功能的抑制作用和对小鼠炎症反应的影响进行了测试。Ircinin抑制眼镜蛇毒液、人滑膜重组体、蜂毒和注射酵母聚糖的大鼠气囊PLA2，其IC50值在微摩尔范围内，与已知抑制剂scalaradial的IC50值相似。另一方面，ircinin对人单核细胞的胞质型PLA2活性较低，并能有效降低人中性粒细胞中白三烯B4（LTB4）的释放。这种海产品对人中性粒细胞功能如超氧化物生成和脱颗粒的影响较弱。在注射酵母聚糖的大鼠气囊中，ircinin在体内抑制渗出液中PLA2的活性，并剂量依赖性地降低髓过氧化物酶水平，而仅在测试的最高剂量下抑制细胞迁移。在小鼠耳水肿试验中局部应用后，该化合物发挥了强大的抗水肿作用。Ircinin是一种新型的PLA2活性抑制剂，我们的结果表明这种海产品作为炎症过程抑制剂具有潜在作用。
