Vassimon C S, Rothschild A M
Department of Pharmacology, Faculty of Medicine, University of São Paulo, Ribeirão Preto, Brazil.
Agents Actions. 1990 Apr;30(1-2):150-2. doi: 10.1007/BF01969024.
Compound 48/80 caused activation of rat mast cell tryptase and chymase along with the release of histamine. Following low speed centrifugation, tryptase remained essentially in the supernatant while chymase sedimented. Enzyme activities as well as histamine release were inhibited by phenylmethyl-sulfonyl fluoride and tosyl-lysine chloromethyl ketone, which are respectively unspecific and specific inhibitors of trypsin-like enzymes. Chymostatin inhibited chymase, but not the release of histamine by 48/80. Tryptase activity thus seems to be essentially involved in the mechanism of histamine release, while chymase activity may be merely one of its accompanying events.
化合物48/80可引起大鼠肥大细胞类胰蛋白酶和糜蛋白酶的激活以及组胺的释放。低速离心后,类胰蛋白酶基本仍留在上清液中,而糜蛋白酶则沉淀下来。苯甲基磺酰氟和甲苯磺酰赖氨酸氯甲基酮分别是非特异性和特异性胰蛋白酶样酶抑制剂,它们可抑制酶活性以及组胺释放。抑糜酶素可抑制糜蛋白酶,但不能抑制48/80引起的组胺释放。因此,类胰蛋白酶活性似乎在组胺释放机制中起主要作用,而糜蛋白酶活性可能仅仅是伴随事件之一。