Santana A, Hyslop S, Antunes E, Mariano M, Bakhle Y S, de Nucci G
Department of Pharmacology, Faculty of Medical Sciences, UNICAMP, Brazil.
Agents Actions. 1993 Jul;39(3-4):104-10. doi: 10.1007/BF01998961.
The inflammatory responses induced by the synthetic polycation poly-L-arginine injected either into the pleural cavity or into the trachea in rats have been investigated. Poly-L-arginine (4-40 nmol/rat) injected intrapleurally induced exudate formation and leucocyte migration (mainly polymorphonuclear cells). The exudate formation (but not cell migration) was dependent on the molecular weight of the poly-L-arginine used (24 and 115 kD). The poly-L-arginine-induced pleurisy was mainly dependent on activation of mast cells since it was significantly reduced either in rats depleted of their stores of histamine and serotonin or in rats previously treated with the serotonin receptor antagonist methysergide. The polyanions heparin and dermatan sulphate when administered intrapleurally with the polycation markedly reduced the exudate formation. Poly-L-arginine (115 kD, 8.5 nmol/rat) injected intratracheally caused lung oedema, increased leucocyte number and protein content of bronchoalveolar lavage, respiratory insufficiency and 60% mortality in 6 h. Depletion of histamine and serotonin stores or of circulating neutrophils decreased the leucocytes in bronchoalveolar lavage but did not increase survival rate, whereas the polyanion dermatan sulphate prevented the mortality completely. These results suggest that the inflammatory changes caused by poly-L-arginine are dependent on mast cell activation but that the lethality after intratracheal administration is due to electrostatic interactions of the polycation with anionic surfaces present in the pulmonary epithelium.
已对合成聚阳离子聚-L-精氨酸注入大鼠胸腔或气管所诱导的炎症反应进行了研究。经胸腔内注射聚-L-精氨酸(4-40 nmol/只大鼠)可诱导渗出液形成和白细胞迁移(主要是多形核细胞)。渗出液形成(而非细胞迁移)取决于所用聚-L-精氨酸的分子量(24和115 kD)。聚-L-精氨酸诱导的胸膜炎主要依赖于肥大细胞的激活,因为在组胺和5-羟色胺储存耗竭的大鼠或先前用5-羟色胺受体拮抗剂麦角新碱治疗的大鼠中,该反应均显著减弱。当与聚阳离子一起经胸腔内给药时,多阴离子肝素和硫酸皮肤素可显著减少渗出液形成。经气管内注射聚-L-精氨酸(115 kD,8.5 nmol/只大鼠)可导致肺水肿、支气管肺泡灌洗中白细胞数量和蛋白质含量增加、呼吸功能不全以及在6小时内死亡率达60%。组胺和5-羟色胺储存耗竭或循环中性粒细胞减少可降低支气管肺泡灌洗中的白细胞数量,但不会提高存活率,而多阴离子硫酸皮肤素可完全防止死亡。这些结果表明,聚-L-精氨酸引起的炎症变化依赖于肥大细胞激活,但气管内给药后的致死性是由于聚阳离子与肺上皮中存在的阴离子表面发生静电相互作用所致。