Faculty of Veterinary Medicine, Department of Veterinary Microbiology, Institute of Preclinical Veterinary Sciences, University of Life Sciences, Lublin, Poland.
Faculty of Biological Sciences, Department of Mycology and Genetics, Institute of Genetics and Microbiology, University of Wroclaw, Wroclaw, Poland.
Mycoses. 2021 May;64(5):537-549. doi: 10.1111/myc.13242. Epub 2021 Jan 28.
Dermatophytoses have gained interest worldwide due to the increased resistance to terbinafine and azoles and difficulty in management of these refractory diseases.
In this study, we identified and analysed Trichophyton mentagrophytes clinical isolates obtained from humans with infections of animal origin.
We used quantitative real-time PCR (qRT-PCR) to examine the transcriptional modulation of three MDR genes (PDR1, MDR2 and MDR4) and analysed squalene epoxidase (SQLE) gene sequences from multidrug-resistant Trichophyton mentagrophytes isolates.
The expression profile revealed a 2- to 12-fold increase in mRNA accumulation in the presence of any of the antifungals, compared to cells incubated without drugs. A statistically significant relationship between the isolates exposed to itraconazole and increased expression of the tested genes was revealed. Substantially lower transcription levels were noted for cells exposed to luliconazole, that is, a third-generation azole. Additionally, in the case of 50% of terbinafine-resistant strains, Leu397Phe substitution in the SQLE gene was detected. Furthermore, the reduced susceptibility to itraconazole and voriconazole was overcome by milbemycin oxime.
In conclusion, our study shed more light on the role of the ABC transporter family in T. mentagrophytes, which, if overexpressed, can confer resistance to single azole drugs and even cross-resistance. Finally, milbemycin oxime could be an interesting compound supporting treatment with azole drugs in the case of refractory dermatomycoses.
由于特比萘芬和唑类药物的耐药性增加以及这些难治性疾病的治疗困难,皮肤癣菌病在全球范围内受到关注。
本研究从动物源性感染患者中分离并分析了亲动物性 Trichophyton mentagrophytes 临床分离株。
我们使用实时荧光定量 PCR (qRT-PCR) 检测了三个多药耐药基因 (PDR1、MDR2 和 MDR4) 的转录调控,并分析了多药耐药性 Trichophyton mentagrophytes 分离株中的 squalene epoxidase (SQLE) 基因序列。
与未孵育药物的细胞相比,在存在任何抗真菌药物的情况下,mRNA 积累的表达谱增加了 2 到 12 倍。暴露于伊曲康唑的分离株与测试基因表达增加之间存在统计学上显著的关系。与第三代唑类药物 luliconazole 相比,细胞的转录水平明显降低。此外,在 50%的特比萘芬耐药株中,检测到 SQLE 基因中 Leu397Phe 取代。此外,milbemycin oxime 克服了对伊曲康唑和伏立康唑的低敏感性。
总之,我们的研究进一步阐明了 ABC 转运蛋白家族在 T. mentagrophytes 中的作用,如果过度表达,它可以赋予对单一唑类药物的耐药性,甚至交叉耐药性。最后,米尔贝肟可能是一种有趣的化合物,可以在难治性皮肤真菌病的情况下支持唑类药物的治疗。