Sarracent J, Finlay C M
Clin Exp Immunol. 1982 Apr;48(1):261-7.
Mouse peritoneal and calf alveolar macrophage cultures were exposed to various concentrations of Clofazimine, 3 (p-chloroanilino)-10-p-Chlorophenyl 2, 10-dihydro-2-isopropylimino, for 120 hr and an increase of four lysosomal enzymes were found with 0 . 3 micrograms/ml of the drug. In mouse peritoneal macrophage cultures, higher concentrations were toxic. Cycloheximide inhibited the lysosomal enzyme activity increase found. No change in enzymatic activity was observed when a lysosomal enriched granular fraction was incubated with various drug concentrations. Our results strongly suggest that Clofazimine at concentrations close to therapeutic serum levels induces de novo synthesis of lysosomal enzymes in macrophage cultures.
将小鼠腹腔和小牛肺泡巨噬细胞培养物暴露于不同浓度的氯法齐明(3-(对氯苯胺基)-10-对氯苯基-2,10-二氢-2-异丙基亚氨基)中120小时,发现当药物浓度为0.3微克/毫升时,四种溶酶体酶的活性增加。在小鼠腹腔巨噬细胞培养物中,较高浓度的药物具有毒性。环己酰亚胺抑制了所发现的溶酶体酶活性的增加。当富含溶酶体的颗粒部分与不同药物浓度一起孵育时,未观察到酶活性的变化。我们的结果强烈表明,接近治疗血清水平的氯法齐明浓度可诱导巨噬细胞培养物中溶酶体酶的从头合成。