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新型磺酰腙衍生物对念珠菌属的体外抗真菌和抗生物膜活性

In vitro antifungal and antibiofilm activities of novel sulfonyl hydrazone derivatives against Candida spp.

作者信息

Aydin Merve, Ozturk Ali, Duran Tugce, Ozmen Ummuhan Ozdemir, Sumlu Esra, Ayan Esra Bilen, Korucu Emine Nedime

机构信息

Department of Medical Microbiology, Faculty of Medicine, KTO Karatay University, Konya, Turkey.

Department of Medical Microbiology, Faculty of Medicine, Niğde Ömer Halisdemir University, Niğde, Turkey.

出版信息

J Mycol Med. 2023 Mar;33(1):101327. doi: 10.1016/j.mycmed.2022.101327. Epub 2022 Aug 18.

Abstract

BACKGROUND

The aim of this study was to investigate the antifungal and antibiofilm activity of the new sulfonyl hydrazones compound derived from sulphonamides.

METHODS

In this study, new sulfonyl hydrazone series were synthesized via a green chemistry method. The structures of the synthesized compounds were characterized by elemental analyses and spectroscopic methods. The antifungal activities of the Anaf compounds against Candida strains under planktonic conditions were tested. The biofilm-forming ability of Candida strains was determined and the inhibitory effects of Anaf compounds on Candida biofilms compared with fluconazole were measured by MTT assay. Expression analysis of biofilm-related genes was investigated with qRT-PCR. The statistical analysis was performed using a one-way ANOVA test. CANDIDA: strains was determined and the inhibitory effects of Anaf compounds on Candida biofilms compared with fluconazole were measured by MTT assay. Expression analysis of biofilm-related genes was investigated with qRT-PCR. The statistical analysis was performed using a one-way ANOVA test.

RESULTS

A total of 16 (45.7%) out of 35 Candida isolates were determined as strong biofilm producers in this study. C. albicans was the most biofilm producer, followed by C. krusei and C. lusitaniae. The Anaf compounds had a broad spectrum of activity with MIC values ranging from 4 μg/ml to 64 μg/ml. Our data indicated that the Anaf compound had a significant effect on inhibiting biofilm formation in both fluconazole-susceptible and -resistant strains. The expression levels of hypha-specific genes als3, hwp1, ece1 and sap5 were downregulated by Anaf compounds.

CONCLUSIONS

Our study revealed that the Anaf compounds had antifungal activity and inhibited fungal biofilms, which may be related to the suppression of C. albicans adherence and hyphal formation. These results suggest that Anaf compounds may have therapeutic potential for the treatment and prevention of biofilm-associated Candida infections.

摘要

背景

本研究旨在探究源自磺胺类药物的新型磺酰腙化合物的抗真菌和抗生物膜活性。

方法

在本研究中,通过绿色化学方法合成了新型磺酰腙系列。合成化合物的结构通过元素分析和光谱方法进行表征。测试了Anaf化合物在浮游条件下对念珠菌菌株的抗真菌活性。测定了念珠菌菌株的生物膜形成能力,并通过MTT法测定了Anaf化合物与氟康唑相比对念珠菌生物膜的抑制作用。用qRT-PCR研究生物膜相关基因的表达分析。使用单向方差分析进行统计分析。测定念珠菌菌株,并通过MTT法测定Anaf化合物与氟康唑相比对念珠菌生物膜的抑制作用。用qRT-PCR研究生物膜相关基因的表达分析。使用单向方差分析进行统计分析。

结果

在本研究中,35株念珠菌分离株中有16株(45.7%)被确定为强生物膜产生菌。白色念珠菌是最主要的生物膜产生菌,其次是克鲁斯念珠菌和葡萄牙念珠菌。Anaf化合物具有广谱活性,MIC值范围为4μg/ml至64μg/ml。我们的数据表明,Anaf化合物对抑制氟康唑敏感和耐药菌株的生物膜形成均有显著作用。Anaf化合物下调了菌丝特异性基因als3、hwp1、ece1和sap5的表达水平。

结论

我们的研究表明,Anaf化合物具有抗真菌活性并抑制真菌生物膜,这可能与抑制白色念珠菌的黏附和菌丝形成有关。这些结果表明,Anaf化合物可能具有治疗和预防生物膜相关念珠菌感染的治疗潜力。

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