Beliavskaia I V, Kukhanova M K, Navashin S M
Antibiotiki. 1976 Mar;21(3):242-5.
It was shown that the mechanism of action of minocycline on intact cells of E. coli was similar to that of oxytetracycline, i.e. specific inhibition of protein synthesis. In acellular systems of synthesis of polyphenylalanine with ribosomes from tetracycline sensitive and resistant strains of E. coli, minocycline and oxytetracycline had close inhibiting activity. Therefore, the highest antimicrobic activity of minocycline was due as compred to oxytetracycline to some advantages at the stage of penetration into the microbial cell and not at the stage the protein synthesis. 4-Epi-oxytetracycline and beta-apo-oxytetracycline possessing competing properties with respect to oxytetracycline at the stage of penetration through the cell membrane did not, however, suppress the synthesis of polyphenylalanine in the acellular system isolated from the sensitive strain of E. coli.
结果表明,米诺环素对完整大肠杆菌细胞的作用机制与土霉素相似,即特异性抑制蛋白质合成。在利用来自四环素敏感和耐药大肠杆菌菌株核糖体的无细胞聚苯丙氨酸合成系统中,米诺环素和土霉素具有相近的抑制活性。因此,与土霉素相比,米诺环素的最高抗菌活性归因于其在穿透微生物细胞阶段的某些优势,而非在蛋白质合成阶段。然而,4-表土霉素和β-去甲土霉素在穿过细胞膜阶段与土霉素具有竞争特性,但它们并未抑制从大肠杆菌敏感菌株分离出的无细胞系统中的聚苯丙氨酸合成。