王丹丹, 时文静, 刘娟娟, 李冰晨, 荆雪宁, 李妍. 新型马来酰亚胺衍生物对白念珠菌的抗生物被膜活性研究J. 药学学报, 2026, 61(2): 504-514. DOI: 10.16438/j.0513-4870.2025-1012
引用本文: 王丹丹, 时文静, 刘娟娟, 李冰晨, 荆雪宁, 李妍. 新型马来酰亚胺衍生物对白念珠菌的抗生物被膜活性研究J. 药学学报, 2026, 61(2): 504-514. DOI: 10.16438/j.0513-4870.2025-1012
WANG Dan-dan, SHI Wen-jing, LIU Juan-juan, LI Bing-chen, JING Xue-ning, LI Yan. The anti-biofilm activity of a novel maleimide derivative against Candida albicansJ. Acta Pharmaceutica Sinica, 2026, 61(2): 504-514. DOI: 10.16438/j.0513-4870.2025-1012
Citation: WANG Dan-dan, SHI Wen-jing, LIU Juan-juan, LI Bing-chen, JING Xue-ning, LI Yan. The anti-biofilm activity of a novel maleimide derivative against Candida albicansJ. Acta Pharmaceutica Sinica, 2026, 61(2): 504-514. DOI: 10.16438/j.0513-4870.2025-1012

新型马来酰亚胺衍生物对白念珠菌的抗生物被膜活性研究

The anti-biofilm activity of a novel maleimide derivative against Candida albicans

  • 摘要: 白念珠菌是临床真菌感染中最常见的条件致病真菌, 其侵袭性致病机制和耐药性与生物被膜的形成密切相关, 因此生物被膜抑制剂的研究具有重要的意义。本研究发现N-(2,4-二甲基苯基)马来酰亚胺(简称IMB-D7) 能够抑制白念珠菌生物被膜的形成, 并对成熟的生物被膜具有一定的清除作用。机制研究发现, IMB-D7显著降低白念珠菌细胞的黏附能力和疏水性、抑制酵母-菌丝相的转换和菌丝的形成, 影响细胞壁成分的含量; IMB-D7能够显著下调与黏附、菌丝形成和细胞壁成分合成相关基因的表达。此外, IMB-D7对人口腔上皮细胞表现出低细胞毒性。因此, 对IMB-D7的深入研究, 有望发现新型抗真菌活性先导分子。

     

    Abstract: Candida albicans (C. albicans) is the most common opportunistic pathogen in clinical fungal infections, and its invasive pathogenic mechanisms and drug resistance are closely associated with biofilm formation. Therefore, research on biofilm inhibitors holds significant importance. This study found that N-(2,4-dimethylphenyl) maleimide (abbreviated as IMB-D7) can inhibit the formation of C. albicans biofilms and has a certain clearance effect on mature biofilms. IMB-D7 significantly reduces the adhesion capacity and hydrophobicity of C. albicans cells, inhibits the yeast-hyphae phase transition and hyphae formation, and affects the content of key components of the cell wall. IMB-D7 significantly downregulates the expression of genes associated with adhesion, hyphal formation, and cell wall component synthesis. Additionally, IMB-D7 exhibits low cytotoxicity toward human oral epithelial cells. Therefore, further research on IMB-D7 holds promise for the discovery of novel antifungal active lead compounds.

     

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