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A40926,一种具有抗奈瑟菌活性的新型糖肽类抗生素。

A40926, a new glycopeptide antibiotic with anti-Neisseria activity.

作者信息

Goldstein B P, Selva E, Gastaldo L, Berti M, Pallanza R, Ripamonti F, Ferrari P, Denaro M, Arioli V, Cassani G

机构信息

Merrell-Dow Research Institute, Lepetit Research Center, Gerenzano, Vares, Italy.

出版信息

Antimicrob Agents Chemother. 1987 Dec;31(12):1961-6. doi: 10.1128/AAC.31.12.1961.

Abstract

In the course of a search for glycopeptide antibiotics having novel biological properties, we isolated A40926. Produced by an actinomycete of the genus Actinomadura, A40926 is a complex of four main factors which contain a fatty acid as part of a glycolipid attached to the peptide backbone. Its activity was, in most respects, similar to that of other glycopeptides, such as vancomycin and teicoplanin. However, in addition to inhibiting gram-positive bacteria, A40926 was very active against Neisseria gonorrhoeae. A40926 was rapidly bactericidal for N. gonorrhoeae clinical isolates at concentrations equal to or slightly higher than the MIC. In mice, levels in serum were higher and more prolonged than those of an equivalent subcutaneous dose of teicoplanin. These properties suggest that A40926 may have potential in the therapy of gonorrhea.

摘要

在寻找具有新型生物学特性的糖肽类抗生素的过程中,我们分离出了A40926。A40926由马杜拉放线菌属的一种放线菌产生,是四种主要成分的复合物,这些成分包含一种脂肪酸,作为与肽骨架相连的糖脂的一部分。在大多数方面,它的活性与其他糖肽类抗生素(如万古霉素和替考拉宁)相似。然而,除了抑制革兰氏阳性菌外,A40926对淋病奈瑟菌也具有很强的活性。在浓度等于或略高于最低抑菌浓度(MIC)时,A40926对淋病奈瑟菌临床分离株具有快速杀菌作用。在小鼠体内,其血清浓度比皮下注射等量替考拉宁时更高且持续时间更长。这些特性表明A40926在淋病治疗中可能具有潜力。

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本文引用的文献

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Vancomycin.
J Antimicrob Chemother. 1984 Dec;14(6):564-7.
3
In vitro activity and human pharmacokinetics of teicoplanin.替考拉宁的体外活性及人体药代动力学
Antimicrob Agents Chemother. 1984 Dec;26(6):881-6. doi: 10.1128/AAC.26.6.881.
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Teicoplanin.替考拉宁
J Antimicrob Chemother. 1984 Nov;14(5):441-5.
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Aridicins, novel glycopeptide antibiotics. II. Isolation and characterization.
J Antibiot (Tokyo). 1985 May;38(5):561-71. doi: 10.7164/antibiotics.38.561.

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