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硫脲衍生物对罗马尼亚分离出的医院菌株的抗真菌和抗氧化活性

Antifungal and Antioxidant Activity of Thiourea Derivatives Against Nosocomial Strains Isolated in Romania.

作者信息

Nedea Ilie Marina Ionela, Bădiceanu Carmellina Daniela, Gheorghe-Barbu Irina, Marinaș Ioana Cristina, Pericleanu Radu, Dragomir Rareș-Ionuț, Dumbravă Andreea Ștefania, Dascălu Ana Maria, Șerban Dragoș, Tudor Corneliu, Solomon Preda Madălina, Popescu Oana, Arsene Andreea Letiția, Velescu Bruno Ștefan

机构信息

Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 6 Traian Vuia Street, 020956 Bucharest, Romania.

Faculty of Biology, University of Bucharest, Intrarea Portocalelor No. 1-3, 060101 Bucharest, Romania.

出版信息

Molecules. 2025 Apr 9;30(8):1675. doi: 10.3390/molecules30081675.

Abstract

Nosocomial fungal infections caused by pose a threat to public health due to their increased resistance to common antifungal drugs. Four thiourea derivatives of 2-thiophenecarboxylic acid were evaluated for their antifungal and antioxidant activity. The antifungal activity of the compounds was tested against strains of isolated from a hospital in Romania. With a notable inhibitory effect on biofilm growth and microbial adherence, the ortho-methylated derivative (SB2) showed the highest antifungal activity. Furthermore, emphasizing the impact of structural factors on the electron-donating capacity of these compounds, antioxidant activity assays (DPPH, FRAP, TEAC and CUPRAC) identified the SB2 compound as having the highest antihemolytic and antioxidant effects. The low cytotoxicity validated by hemocompatibility assays makes these compounds options for antifungal treatment. The results show that antifungal and antioxidant action is greatly influenced by structural modifications, especially the position of the methyl group on the aromatic ring. The possible clinical uses of these molecules as drugs for the treatment of multidrug-resistant infections needs further investigation.

摘要

由……引起的医院获得性真菌感染因其对常见抗真菌药物的耐药性增加而对公共卫生构成威胁。对2-噻吩羧酸的四种硫脲衍生物的抗真菌和抗氧化活性进行了评估。测试了这些化合物对从罗马尼亚一家医院分离出的……菌株的抗真菌活性。邻甲基化衍生物(SB2)对生物膜生长和微生物黏附具有显著抑制作用,显示出最高的抗真菌活性。此外,抗氧化活性测定(DPPH、FRAP、TEAC和CUPRAC)强调了结构因素对这些化合物供电子能力的影响,确定SB2化合物具有最高的抗溶血和抗氧化作用。血液相容性测定验证的低细胞毒性使这些化合物成为抗真菌治疗的选择。结果表明,抗真菌和抗氧化作用受结构修饰的极大影响,尤其是芳香环上甲基的位置。这些分子作为治疗多重耐药……感染的药物的可能临床用途需要进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/acfb/12029497/a52766a91f7d/molecules-30-01675-g001a.jpg

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