Asuquo A E, Piddock L J
Department of Infection, Medical School, University of Birmingham, Edgbaston, UK.
J Antimicrob Chemother. 1993 Jun;31(6):865-80. doi: 10.1093/jac/31.6.865.
The accumulation of fifteen quinolone antimicrobial agents (nalidixic acid, eight mono-fluorinated agents, three di-fluorinated agents and three tri-fluorinated agents) by Escherichia coli KL16, Staphylococcus aureus NCTC 8532 and Pseudomonas aeruginosa NCTC 10662 was studied. The concentration of quinolones accumulated varied with the quinolone and the bacterial species, and was not affected by the number of fluorine atoms on the quinolone nucleus. There was also no direct relationship between the hydrophobicity or the molecular size of each drug and accumulation or activity. The killing of the three strains by the fifteen quinolones at a concentration of 10 mg/L was determined in broth and phosphate buffer to mimic the conditions of the accumulation assay. The bactericidal activity varied with the agent and the strain, and usually reflected the in-vitro activity of the drug. Despite most agents causing a decrease in the viable count of the three strains there was no detectable effect on the pattern of accumulation of the quinolones.
研究了大肠杆菌KL16、金黄色葡萄球菌NCTC 8532和铜绿假单胞菌NCTC 10662对15种喹诺酮类抗菌剂(萘啶酸、8种单氟代剂、3种二氟代剂和3种三氟代剂)的蓄积情况。蓄积的喹诺酮类药物浓度因喹诺酮类药物和细菌种类而异,且不受喹诺酮核上氟原子数量的影响。每种药物的疏水性或分子大小与蓄积或活性之间也没有直接关系。在肉汤和磷酸盐缓冲液中测定了15种喹诺酮类药物在10 mg/L浓度下对这三种菌株的杀灭情况,以模拟蓄积试验的条件。杀菌活性因药物和菌株而异,通常反映了药物的体外活性。尽管大多数药物导致这三种菌株的活菌数减少,但对喹诺酮类药物的蓄积模式没有可检测到的影响。