Sompolinsky D, Krausz J
Antimicrob Agents Chemother. 1973 Sep;4(3):237-47. doi: 10.1128/AAC.4.3.237.
The relative growth inhibition caused by 12 tetracyclines in a susceptible strain of Staphylococcus aureus (111-elim) and in the same strain carrying a resistance-plasmid (111) showed entirely different patterns. For four of the tetracyclines (minocycline, anhydrotetracycline, chelocardin, and desdimethylaminotetracycline), the strain with the tetracycline plasmid (111) had virtually the same tolerance as the susceptible strain (111-elim). A resistant mutant of strain 111-elim showed a third pattern of relative growth inhibition, and another distinct pattern was observed in a veterinary wild strain of S. aureus. Of the 12 tetracyclines, 11 were effective inducers of higher tetracycline resistance in S. aureus 111, but no correlation was found between the efficacy of the tetracyclines as inducers and as inhibitors of growth of 111-elim or 111. At external drug concentrations causing doubling of the generation time (K(i)), 111-elim accumulated tetracycline, oxytetracycline, and minocycline to a degree corresponding to several thousand molecules per coccus. At a fixed external drug concentration, 111 accumulated less tetracycline and oxytetracycline than 111-elim, whereas comparison at their respective K(i) values showed accumulation to be significantly higher for 111 than for 111-elim. The accumulation of tetracyclines is assumed to involve both surface sorption and active membrane transport. Resistance is probably due to decreased accumulation of the drugs, and a hypothesis explaining the mechanism of resistance is offered.
12种四环素类药物对金黄色葡萄球菌敏感菌株(111-elim)及其携带耐药质粒的同一菌株(111)所引起的相对生长抑制呈现出完全不同的模式。对于其中4种四环素类药物(米诺环素、脱水四环素、氯卡环素和去二甲氨基四环素),携带四环素质粒的菌株(111)与敏感菌株(111-elim)的耐受性几乎相同。111-elim菌株的一个耐药突变体呈现出第三种相对生长抑制模式,并且在一株金黄色葡萄球菌兽医野生菌株中观察到了另一种不同的模式。在这12种四环素类药物中,有11种是金黄色葡萄球菌111中更高四环素耐药性的有效诱导剂,但四环素类药物作为诱导剂的效力与其对111-elim或111生长的抑制效力之间未发现相关性。在导致世代时间加倍的外部药物浓度(K(i))下,111-elim积累四环素、土霉素和米诺环素的程度相当于每个球菌数千个分子。在固定的外部药物浓度下,111积累的四环素和土霉素比111-elim少,而在它们各自的K(i)值下进行比较显示,111的积累量显著高于111-elim。四环素类药物的积累被认为涉及表面吸附和主动膜转运。耐药性可能是由于药物积累减少所致,并提出了一个解释耐药机制的假说。