Nakae R, Nakae T
Antimicrob Agents Chemother. 1982 Oct;22(4):554-9. doi: 10.1128/AAC.22.4.554.
The diffusion of aminoglycoside antibiotics (gentamicin, kanamycin, streptomycin, fradiomycin, lividomycin, and mannosylparomomycin) through porin pores was examined in vitro by the liposome swelling technique, using vesicle membranes reconstituted from phospholipids and purified porin trimers. Results showed that aminoglycoside antibiotics diffuse through porin-pores very efficiently, as rapidly as hexoses and disaccharides, despite the fact that the molecular weights of the aminoglycosides used were higher than or close to the exclusion limit of porin pores. The susceptibility to aminoglycoside antibiotics of mutant strains producing 3 to 4% of porin was not significantly different from that of a strain producing a wild-type quantity of porin. These results were interpreted to mean that aminoglycoside antibiotics diffuse through porin-pores very efficiently. Therefore, the diffusion of these drugs through the mutant outer membranes producing 3 to 4% of porin is not a rate-limiting step for aminoglycoside diffusion and its action.
采用脂质体膨胀技术，通过由磷脂和纯化的孔蛋白三聚体重构的囊泡膜，在体外研究了氨基糖苷类抗生素（庆大霉素、卡那霉素、链霉素、弗氏霉素、青紫霉素和甘露糖基巴龙霉素）通过孔蛋白孔的扩散情况。结果表明，氨基糖苷类抗生素能非常有效地通过孔蛋白孔扩散，速度与己糖和二糖一样快，尽管所用氨基糖苷类药物的分子量高于或接近孔蛋白孔的排阻极限。产生3%至4%孔蛋白的突变菌株对氨基糖苷类抗生素的敏感性与产生野生型数量孔蛋白的菌株没有显著差异。这些结果被解释为意味着氨基糖苷类抗生素能非常有效地通过孔蛋白孔扩散。因此，这些药物通过产生3%至4%孔蛋白的突变体外膜的扩散不是氨基糖苷类扩散及其作用的限速步骤。
