Nakagawa H, Shuto K, Isaji M, Watanabe K, Tsurufuji S
J Pharmacobiodyn. 1981 Jun;4(6):429-35. doi: 10.1248/bpb1978.4.429.
Effect of proteinase inhibitors on the carrageenin-induced inflammation was studied. The formation of granulation tissue was markedly inhibited by a single injection of epsilon-amino-n-caproic acid n-hexyl ester (EACA hexyl ester, 300 mg/kg) into the carrageenin-airpouch immediately after carrageenin injection, whereas repeated injections of the inhibitor starting at 12 hr, 24 hr and 48 hr after carrageenin injection were less effective, slightly effective and ineffective, respectively. A dose-dependent inhibition of both the formation of granulation tissue and the migration of polymorphonuclear leukocytes (PMNs) into the inflammatory locus was found by a single injection of EACA hexyl ester into the carrageenin-airpouch immediately after carrageenin injection. Similarly, a single injection of L-1-tosylamide-2-phenylethyl chloromethyl ketone (TPCK, 50 mg/kg) and N-alpha-p-tosyl-L-lysine chloromethyl ketone (TLCK, 30 mg/kg) inhibited both the formation of granulation tissue and the migration of PMNs into the inflammatory locus. These results suggest that serine proteinase inhibitors such as EACA hexyl ester, TPCK and TLCK exert their anti-inflammatory actions by interfering with the initial inflammatory reactions including the migration of PMNs into inflammatory locus after carrageenin injection.
研究了蛋白酶抑制剂对角叉菜胶诱导的炎症的影响。在注射角叉菜胶后立即向角叉菜胶气囊肿内单次注射ε-氨基己酸正己酯（EACA己酯，300mg/kg），可显著抑制肉芽组织的形成，而在注射角叉菜胶后12小时、24小时和48小时开始重复注射该抑制剂，其效果分别为较差、稍有效和无效。在注射角叉菜胶后立即向角叉菜胶气囊肿内单次注射EACA己酯，发现对肉芽组织形成和多形核白细胞（PMN）向炎症部位的迁移均有剂量依赖性抑制作用。同样，单次注射L-1-对甲苯磺酰胺-2-苯乙基氯甲基酮（TPCK，50mg/kg）和N-α-对甲苯磺酰-L-赖氨酸氯甲基酮（TLCK，30mg/kg）可抑制肉芽组织的形成和PMN向炎症部位的迁移。这些结果表明，丝氨酸蛋白酶抑制剂如EACA己酯、TPCK和TLCK通过干扰初始炎症反应发挥其抗炎作用，这些初始炎症反应包括注射角叉菜胶后PMN向炎症部位的迁移。
