Kivman G Ia, Guliaev A E, Nigmatulin A Z, Nadirova B A
Antibiotiki. 1984 Jan;29(1):35-9.
The studies showed that the tetracyclines tested (morphocycline, tetracycline and methacycline) penetrated into leucocytes of the human peripheral blood. Agranulocyte absorbed the drugs more actively than granulocytes. Pinocytosis was suggested to be involved in the penetration. On interaction with intracellular structures the tetracyclines reversibly bound to the organoid cells lost their biological activity to a significant degree. Progressive dissociation of organoid-drug complexes and the egress of tetracyclines from the cells were likely to occur as their contents in the extracellular environment decreased. The penetration capacity and subcellular structure affinity of methacycline were the highest among the drugs tested. It is suggested that penetration of the tetracyclines through the cytoplasmic membranes and their distribution inside the cells are reciprocal.
研究表明，所测试的四环素类药物（吗啉环素、四环素和甲烯土霉素）可渗透进入人外周血白细胞。无粒细胞比粒细胞更积极地吸收这些药物。据推测，胞饮作用参与了药物的渗透过程。四环素类药物与细胞内结构相互作用时，可逆地结合到类器官细胞上，在很大程度上丧失了其生物活性。随着细胞外环境中四环素类药物含量的降低，类器官 - 药物复合物可能会逐渐解离，四环素类药物也可能从细胞中排出。在所测试的药物中，甲烯土霉素的渗透能力和对亚细胞结构的亲和力最高。有人提出，四环素类药物穿过细胞质膜的渗透及其在细胞内的分布是相互关联的。
