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新型三唑类药物D0870与其他四种抗真菌药物对念珠菌和光滑球拟酵母菌临床分离株的抗真菌活性比较。

Antifungal activity of a new triazole, D0870, compared with four other antifungal agents tested against clinical isolates of Candida and Torulopsis glabrata.

作者信息

Pfaller M A, Bale M J, Buschelman B, Rhomberg P

机构信息

Department of Pathology, University of Iowa College of Medicine, Iowa City 52242.

出版信息

Diagn Microbiol Infect Dis. 1994 Jun;19(2):75-80. doi: 10.1016/0732-8893(94)90116-3.

Abstract

D0870 is a new triazole agent with potent, broad-spectrum antifungal activity. We investigated the in vitro activity of D0870, fluconazole, itraconazole, amphotericin B, and 5-fluorocytosine (5FC) against 319 clinical isolates of Candida spp. and Torulopsis glabrata. In vitro susceptibility testing was performed using a microdilution broth method performed according to NCCLS guidelines. D0870 was very active (MIC90 of 0.12 microgram/ml and 0.5 microgram/ml at 24 and 48 h incubation, respectively) against all of the yeast isolates. D0870 was 2- to 32-fold more active than amphotericin B and 2- to 8500-fold more active than 5FC. By comparison with the other triazoles, D0870 was generally 2- to 16-fold more active than itraconazole and > or = 16-fold more active than fluconazole. More than half (53%) of C. albicans isolates with elevated fluconazole and itraconazole MICs (> or = 128 micrograms/ml and > 8.0 micrograms/ml, respectively) were inhibited by < or = 1.0 microgram/ml of D0870. Based on these studies, D0870 has promising antifungal activity and warrants further in vitro and in vivo investigation.

摘要

D0870是一种新型三唑类药物,具有强大的广谱抗真菌活性。我们研究了D0870、氟康唑、伊曲康唑、两性霉素B和5-氟胞嘧啶(5FC)对319株念珠菌属和光滑球拟酵母菌临床分离株的体外活性。体外药敏试验采用根据美国国家临床实验室标准委员会(NCCLS)指南进行的微量肉汤稀释法。D0870对所有酵母分离株都非常有效(在孵育24小时和48小时时,MIC90分别为0.12微克/毫升和0.5微克/毫升)。D0870的活性比两性霉素B高2至32倍,比5FC高2至8500倍。与其他三唑类药物相比,D0870的活性通常比伊曲康唑高2至16倍,比氟康唑高≥16倍。超过一半(53%)氟康唑和伊曲康唑MIC升高(分别≥128微克/毫升和>8.0微克/毫升)的白色念珠菌分离株被≤1.0微克/毫升的D0870抑制。基于这些研究,D0870具有良好的抗真菌活性,值得进一步进行体外和体内研究。

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