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[氯喹单次及重复给药对大鼠肝细胞溶酶体蛋白酶活性的影响]

[The effect of single and repeated administration of chloroquine on the activity of lysosomal proteinases in rat liver cells].

作者信息

Korolenko T A, Rukavishnikova E V, Pupyshev A B

出版信息

Vopr Med Khim. 1990 Nov-Dec;36(6):20-3.

PMID:2075715
Abstract

Effects of single and repeated injections of lysosomotropic agent chloroquine on lysosomal proteolytic activity and physico-chemical properties of rat liver lysosomes have been studied. Chloroquine was administered intraperitoneally to rats at a dose of 30 mg/kg of body mass. Osmotic properties, lysosomal enzymes activity and functional state of the system of mononuclear phagocytes were estimated. No alterations of colloid carbon clearance followed by a single dose of chloroquine administration were noted. Distinct alterations in osmotic properties, weak labilization of lysosomes and an increase in acid hydrolases activity were similar after single and/or repeated chloroquine administrations, whereas activation of cysteine proteinases and cathepsin D were most pronounced. Chloroquine accumulation by rat liver cells proved to be similar, but the drug excretion was longer after repeated injections. The lysosomal disorders noted were similar to those symptoms of lysosomal storage disease.

摘要

研究了单次和重复注射溶酶体促透剂氯喹对大鼠肝脏溶酶体溶酶体蛋白水解活性和理化性质的影响。以30mg/kg体重的剂量给大鼠腹腔注射氯喹。评估了单核吞噬细胞系统的渗透特性、溶酶体酶活性和功能状态。单次给予氯喹后,未观察到胶体碳清除率的改变。单次和/或重复给予氯喹后,渗透特性的明显改变、溶酶体的轻度不稳定和酸性水解酶活性的增加相似,而半胱氨酸蛋白酶和组织蛋白酶D的激活最为明显。大鼠肝细胞对氯喹的蓄积相似,但重复注射后药物排泄时间延长。观察到的溶酶体紊乱与溶酶体贮积病的症状相似。

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