Kuck N A, Forbes M
Antimicrob Agents Chemother. 1973 Jun;3(6):662-4. doi: 10.1128/AAC.3.6.662.
Minocycline (7-dimethylamino-6-demethyl-6-deoxytetracycline) is a new semisynthetic tetracycline with potent activity against tetracycline-susceptible bacterial pathogens and unique activity against tetracycline-resistant staphylococci. Studies to determine the basis for this unique activity showed that, whereas tetracycline-resistant staphylococci took up less (3)H-tetracycline than the susceptible cells, both the tetracycline-resistant and -susceptible cells accumulated equivalent amounts of (14)C-minocycline. In contrast, tetracycline-resistant Escherichia coli cells were relatively resistant to minocycline and accumulated less of both drugs than did the susceptible organisms. It is proposed that minocycline is effective against tetracycline-resistant staphylococci because of its ability to penetrate the cells sufficiently to reach inhibiting concentrations at sensitive reaction sites.
米诺环素(7-二甲氨基-6-去甲基-6-脱氧四环素)是一种新型半合成四环素,对四环素敏感的细菌病原体具有强大活性,对四环素耐药葡萄球菌具有独特活性。确定这种独特活性基础的研究表明,虽然四环素耐药葡萄球菌摄取的(3)H-四环素比敏感细胞少,但四环素耐药和敏感细胞积累的(14)C-米诺环素量相当。相比之下,四环素耐药大肠杆菌细胞对米诺环素相对耐药,积累的两种药物都比敏感菌少。有人提出,米诺环素对四环素耐药葡萄球菌有效是因为它有足够的能力穿透细胞,在敏感反应位点达到抑制浓度。