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酮康唑对念珠菌菌株产生的天冬酰胺蛋白酶活性的影响。

The influence of ketoconazole on the activity of asparagine protease produced by Candida strains.

作者信息

Kurnatowski Piotr, Grabek Arkadiusz

机构信息

Department of Biology and Medical Parasitology, Medical University of L6di, Hallera 1, Lódź, Poland.

出版信息

Res Commun Mol Pathol Pharmacol. 2004;115-116:265-76.

Abstract

The investigations concerning the activity of antimycotic drugs on pathogenic fungi, revealed a decrease of sensitivity of fungi, especially of the Candida species. In other investigations we have stated that strains isolated from patients have other than standard enzymatic activity. So it seems to be interesting to have evaluated the model for analysis in vitro the influence of antimycotic drug for egzoenzyme of fungi. The aims of the study were: 1. estimation of the influence in vitro ketoconazole, which was added everyday for 3 weeks on curves of activity of the drug, on strains isolated from patients; 2. estimation of asparagine protease activity on strains before, during and after the added drug to the culture. During the study we evaluated the model in vitro to obtain strains with lower sensitivity for a antimycotic drug. Everyday during a 3 week period we added to the culture ketoconazole in the concentration of about 2, 4 and 6 times higher than the minimal inhibitory concentration (MIC). Before, 1, 2 and 3 weeks after we investigated the activity of asparaginee protease. We obtained the following results: 1. Ketoconazole added to the culture of Candida strains during 3 weeks had influenced the response curves, which was observed as statistical significant changes between MIC values. 2. Ketoconazole after 1 week of administration decreased and after 2 and 3 weeks increased of asparagine protease activity.

摘要

关于抗真菌药物对致病真菌活性的研究表明,真菌尤其是念珠菌属的敏感性有所下降。在其他研究中我们指出,从患者分离出的菌株具有非标准的酶活性。因此,评估体外分析抗真菌药物对真菌胞外酶影响的模型似乎很有意思。本研究的目的是:1. 评估每天添加酮康唑3周对从患者分离出的菌株的药物活性曲线的体外影响;2. 评估在向培养物中添加药物之前、期间和之后菌株中天冬酰胺蛋白酶的活性。在研究过程中,我们评估了体外模型,以获得对抗真菌药物敏感性较低的菌株。在3周的时间里,每天我们向培养物中添加浓度约为最低抑菌浓度(MIC)2倍、4倍和6倍的酮康唑。在添加药物之前、1周后、2周后和3周后,我们研究了天冬酰胺蛋白酶的活性。我们得到了以下结果:1. 在3周内添加到念珠菌菌株培养物中的酮康唑影响了反应曲线,这表现为MIC值之间的统计学显著变化;2. 酮康唑给药1周后天冬酰胺蛋白酶活性降低,给药2周和3周后活性增加。

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