Nakagawa H, Suzuki M, Shuto K, Watanabe K, Iwata K, Isaji M, Tsurufuji S
J Pharmacobiodyn. 1982 May;5(5):319-27. doi: 10.1248/bpb1978.5.319.
Gelatinase, elastase and cathepsin G isolated from the granule extract of rat polymorphonuclear leukocytes (PMNs) had similar properties to the enzymes of human PMNs already reported. Effect of proteinase inhibitors on these neutral proteinases isolated from rat PMNs was studied. Epsilon-Amino-n-caproic acid n-hexyl ester, a proteinase inhibitor having anti-inflammatory activity, inhibited cathepsin G, whereas elastase was activated by the inhibitor. On the other hand, leupeptin, L-1-tosylamide-2-phenylethyl chloromethyl ketone and N-alpha-p-tosyl-L-lysine chloromethyl ketone, which had been reported as anti-inflammatory inhibitors, had no inhibitory effect on these neutral proteinases. These results suggest that proteinase inhibitors reported as anti-inflammatory agents exert their anti-inflammatory actions not by direct inhibition of the neutral proteinases released from PMNs, but by other effects such as suppression of the infiltration of PMNs into inflammatory locus.
从大鼠多形核白细胞（PMNs）颗粒提取物中分离出的明胶酶、弹性蛋白酶和组织蛋白酶G，其性质与已报道的人PMNs中的酶相似。研究了蛋白酶抑制剂对从大鼠PMNs中分离出的这些中性蛋白酶的作用。具有抗炎活性的蛋白酶抑制剂ε-氨基-n-己酸正己酯可抑制组织蛋白酶G，而弹性蛋白酶则被该抑制剂激活。另一方面，已报道具有抗炎作用的亮抑酶肽、L-1-对甲苯磺酰胺-2-苯乙基氯甲基酮和N-α-对甲苯磺酰-L-赖氨酸氯甲基酮，对这些中性蛋白酶没有抑制作用。这些结果表明，被报道为抗炎剂的蛋白酶抑制剂并非通过直接抑制从PMNs释放的中性蛋白酶来发挥其抗炎作用，而是通过其他作用，如抑制PMNs向炎症部位的浸润。
