[利福平与大鼠肝细胞类器官的相互作用及其细胞内分布]。

Antibiotiki Pub Date : 1984-11-01
A E Guliaev, G Ia Kivman
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引用次数: 0

摘要

研究了利福平与分离的大鼠肝脏亚细胞组分的相互作用(复合物的结合和解离)和抗生素的细胞内分布,主要类器官以接近肝细胞成分的自然体积比的比例存在。细胞核和线粒体在药物结合过程中最为活跃。微粒体就不那么重要了。利福平与类器官形成可移动的配合物,并且很容易从亚细胞组分中释放出来,在洗涤后恢复其活性。细胞内分布如下:37.7%的活性利福平积聚在细胞质中,其余的利福平可逆地结合在细胞核、线粒体和微粒体的部分中。利福平的细胞药代动力学特征,即在细胞质中的显著浓度,可能沉积在亚细胞结构中,同时恢复活性的能力,可能定义了这种抗生素在细胞内微生物方面的抗菌潜力。
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[Interaction of rifampicin with hepatocyte organoids in rats and its intracellular distribution].

Interaction of rifampicin with isolated subcellular fractions of the rat liver (binding and dissociation of the complexes) and intracellular distribution of the antibiotic were studied in the presence of the main organoids taken in the ratio close to the natural volume ratio of the hepatocyte cell components. The nuclei and mitochondria were most active during drug binding. The microsomes were less important. Rifampicin formed mobile complexes with organoids and was easily released from the subcellular fractions recovering its activity on washing. The intracellular distribution was the following: 37.7 per cent of rifampicin in the active form was accumulated in cytosol and the remaining amount was reversibly bound in the fractions of the nuclei, mitochondria and microsomes. The characteristic features of the cell pharmacokinetics of rifampicin, i.e. significant concentration in cytosol, possible deposition in the subcellular structures and at the same time the capacity for recovery of the activity might define the antimicrobial potential of this antibiotic in respect to the intracellular microorganisms.

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