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西托环素,四环素类似物:抗菌活性、血清结合、脂溶性及细菌摄取的体外研究

Cetocycline, tetracycline analog: in vitro studies of antimicrobial activity, serum binding, lipid solubility, and uptake by bacteria.

作者信息

Proctor R, Craig W, Kunin C

出版信息

Antimicrob Agents Chemother. 1978 Apr;13(4):598-604. doi: 10.1128/AAC.13.4.598.

Abstract

Cetocycline (formerly chelocardin or cetotetrine) is structurally related to the tetracyclines. It was found to be more active than tetracycline against many clinical isolates of aerobic gram-negative bacilli, but is less active against staphylococci, and has no activity against Pseudomonas. It is bactericidal against susceptible enteric gram-negative bacteria at concentrations two to four times higher than the minimal inhibiting concentrations. The drug is highly lipid soluble; more than 80% is bound to serum, and it is more avidly taken up by susceptible bacteria than tetracycline. A direct correlation between drug uptake and susceptibility of bacteria was not noted, except with a strain of Proteus vulgaris.

摘要

西托环素(曾用名螯合菌素或西托四环素)在结构上与四环素相关。已发现它对许多需氧革兰氏阴性杆菌临床分离株的活性比四环素更强,但对葡萄球菌的活性较弱,且对铜绿假单胞菌无活性。在浓度比最低抑菌浓度高两到四倍时,它对敏感的肠道革兰氏阴性菌具有杀菌作用。该药具有高度脂溶性;超过80%与血清结合,且与四环素相比,敏感细菌对它的摄取更迅速。除了普通变形杆菌菌株外,未发现药物摄取与细菌敏感性之间存在直接相关性。

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