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新型氨基糖苷类药物sporaricin A的体外和体内抗菌活性

In vitro and in vivo antimicrobial activities of sporaricin A, a new aminoglycoside.

作者信息

Kobayashi F, Saino Y, Koshi T, Hattori Y

出版信息

Antimicrob Agents Chemother. 1980 Mar;17(3):337-43. doi: 10.1128/AAC.17.3.337.

Abstract

The in vitro and in vivo antimicrobial activity of sporaricin A, a new aminoglycoside, was compared with that of amikacin, dibekacin, and gentamicin. Sporaricin A showed a broad spectrum of activity against various gram-positive and -negative bacteria, including amikacin-, dibekacin-, or gentamicin-resistant strains. Sporaricin A inhibited more than 90% of clinical isolates of staphylococci, Klebsiella, Enterobacter, Citrobacter, Serratia, and Proteus, except for P. morganii and P. inconstans, at the concentration of 3.13 microgram/ml. This activity, except for that against Serratia, was similar to that of amikacin. Against P. inconstans and S. marcescens, sporaricin A was more effective than amikacin, dibekacin, and gentamicin. However, its activity against Pseudomonas aeruginosa was relatively weak in comparison with three other aminoglycosides. Sporaricin A was highly effective against bacteria that had various aminoglycoside-inactivating enzymes and that were resistant to the other drugs tested, but it was not active against those with aminoglycoside 3-acetyltransferase-I. The activity of sporaricin A tended to be greater with a reduction in inoculum size of bacteria and an increase in medium pH and decreased slightly in the presence of 10 to 50% horse serum. The in vitro activity was confirmed by in vivo tests in experimental infections with various bacteria. Its protective effect seemed to be equal to or greater than that of amikacin or dibekacin.

摘要

将新型氨基糖苷类药物孢霉素A的体外和体内抗菌活性与阿米卡星、地贝卡星和庆大霉素进行了比较。孢霉素A对各种革兰氏阳性菌和阴性菌具有广谱活性,包括对阿米卡星、地贝卡星或庆大霉素耐药的菌株。在浓度为3.13微克/毫升时,孢霉素A抑制了超过90%的葡萄球菌、克雷伯菌、肠杆菌、柠檬酸杆菌、沙雷菌和变形杆菌的临床分离株,但摩根氏变形杆菌和殊异变形杆菌除外。除对沙雷菌的活性外,该活性与阿米卡星相似。对于殊异变形杆菌和粘质沙雷菌,孢霉素A比阿米卡星、地贝卡星和庆大霉素更有效。然而,与其他三种氨基糖苷类药物相比,其对铜绿假单胞菌的活性相对较弱。孢霉素A对具有各种氨基糖苷类失活酶且对其他测试药物耐药的细菌高度有效,但对具有氨基糖苷3-乙酰转移酶-I的细菌无活性。随着细菌接种量的减少、培养基pH值的升高,孢霉素A的活性趋于增强,在存在10%至50%马血清的情况下活性略有下降。通过对各种细菌进行实验感染的体内试验证实了其体外活性。其保护作用似乎等于或大于阿米卡星或地贝卡星。

相似文献

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In vitro comparison of dibekacin and gentamicin activities.地贝卡星与庆大霉素活性的体外比较。
Antimicrob Agents Chemother. 1981 Jan;19(1):190-2. doi: 10.1128/AAC.19.1.190.

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Phosphorylated inactivation of aminoglycosidic antibiotics by Pseudomonas aeruginosa.
Jpn J Microbiol. 1971 May;15(3):265-72. doi: 10.1111/j.1348-0421.1971.tb00578.x.

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