Kubera Dominika, Sławińska-Brych Adrianna, Dróźdż Agnieszka, Olender Alina, Bogut Agnieszka, Matwijczuk Arkadiusz, Karcz Dariusz, Kimsa-Dudek Magdalena, Gola Joanna Magdalena, Kruszniewska-Rajs Celina, Adamska Jolanta, Szukała Magdalena, Dąbrowski Wojciech, Stepulak Andrzej, Gagoś Mariusz
Department of Cell Biology, Maria Curie-Sklodowska University, Akademicka 19, 20-033, Lublin, Poland.
Faculty of Physics and Applied Computer Science, AGH University of Krakow, al. A. Mickiewicza 30, 30-059, Krakow, Poland.
Sci Rep. 2025 May 13;15(1):16663. doi: 10.1038/s41598-025-01075-2.
Amphotericin B (AmB) is a potent antifungal agent with minimal resistance among clinical isolates, but its use is limited by severe side effects. Reducing its toxicity through combination therapy with synergistic compounds is a promising strategy. This study investigates the antifungal potential of 1,3,4-thiadiazole derivatives, focusing on AT2 and AT10, against Candida species. AT2 demonstrated the highest activity, achieving complete inhibition at 128 µg/mL and notable suppression at lower concentrations. The combination of AT2 and AT10 with amphotericin B exhibited synergistic effects, leading to significant structural alterations in the fungal cell wall, including reduced β-glucan levels and increased synthesis of mannan and phosphomannan. These modifications correlated with enhanced antifungal efficacy without exacerbating cytotoxicity toward human fibroblasts and renal epithelial cells. The spectroscopic analysis suggested that the synergy arose from both cell wall disruptions and amphotericin B disaggregation. These findings highlight the potential of thiadiazole-based combination therapies for combating resistant fungal infections.
两性霉素B(AmB)是一种强效抗真菌剂,临床分离株对其耐药性极小,但其使用受到严重副作用的限制。通过与具有协同作用的化合物联合治疗来降低其毒性是一种很有前景的策略。本研究调查了1,3,4-噻二唑衍生物(重点是AT2和AT10)对念珠菌属的抗真菌潜力。AT2表现出最高的活性,在128µg/mL时实现完全抑制,在较低浓度时也有显著抑制作用。AT2和AT10与两性霉素B联合使用表现出协同作用,导致真菌细胞壁发生显著结构改变,包括β-葡聚糖水平降低以及甘露聚糖和磷酸甘露聚糖合成增加。这些修饰与增强的抗真菌功效相关,而不会加剧对人成纤维细胞和肾上皮细胞的细胞毒性。光谱分析表明,协同作用源于细胞壁破坏和两性霉素B解聚。这些发现突出了基于噻二唑的联合疗法对抗耐药真菌感染的潜力。