Kivman G Ia, Nadirova B A, Guliaev A E
Antibiotiki. 1982 Jan;27(1):45-8.
Binding of tetracyclines, i. e. tetracycline, oxytetracycline, morphocycline, methacycline and doxycycline by subcellular fractions of rat liver homogenates was studied on randombred albino rats. It was shown that the drugs lost their activity to a significant extent on contact with nuclei, mitochondria, microsomes and the fraction mixtures. The mitochondrial fraction bound the highest amounts of the drugs. The binding level of methacycline by the organoids was the highest, while that of morphocycline was the least. Binding of the tetracyclines with the subcellular fractions of the liver was to a certain extent reversible. Accumulation of the antibiotic in the cells may be advantageous from the viewpoint of its effect on the intracellular microbes if possible subsequent dissociation from its complex with organoids is considered. At the same time the mitochondriatropic properties of the tetracyclines may be the basis for their toxic effect on the host cells.
在随机繁殖的白化大鼠上研究了四环素类药物，即四环素、土霉素、金霉素、甲烯土霉素和强力霉素与大鼠肝脏匀浆亚细胞组分的结合情况。结果表明，这些药物在与细胞核、线粒体、微粒体及组分混合物接触时会在很大程度上丧失活性。线粒体组分结合的药物量最多。类器官对甲烯土霉素的结合水平最高，而对金霉素的结合水平最低。四环素类药物与肝脏亚细胞组分的结合在一定程度上是可逆的。如果考虑到抗生素随后可能从其与类器官的复合物中解离，那么从其对细胞内微生物的作用角度来看，抗生素在细胞内的积累可能是有利的。同时，四环素类药物的亲线粒体特性可能是其对宿主细胞产生毒性作用的基础。
