Medical and Molecular Mycology Laboratory, Department of Clinical and Toxicological Analyses, Federal University of Rio Grande do Norte, Natal, Brazil.
Department of Pharmacy, Federal University of Rio Grande do Norte, Natal, Brazil.
PLoS One. 2024 Aug 13;19(8):e0303878. doi: 10.1371/journal.pone.0303878. eCollection 2024.
The limited arsenal of antifungal drugs have prompted the search for novel molecules with biological activity. This study aimed to characterize the antifungal mechanism of action of Eugenia uniflora extract and its synergistic activity with commercially available antifungal drugs on the following Candida species: C. albicans, C. tropicalis, C. glabrata, C. parapsilosis and C. dubliniensis. In silico analysis was performed to predict antifungal activity of the major compounds present in the extract. Minimal inhibitory concentrations (MICs) were determined in the presence of exogenous ergosterol and sorbitol. Yeast cells were grown in the presence of stressors. The loss of membrane integrity was assessed using propidium iodide staining (fluorescence emission). Synergism between the extract and antifungal compounds (in addition to time kill-curves) was determined. Molecular docking revealed possible interactions between myricitrin and acid gallic and enzymes involved in ergosterol and cell wall biosynthesis. Candida cells grown in the presence of the extract with addition of exogenous ergosterol and sorbitol showed 2 to 8-fold increased MICs. Strains treated with the extract revealed greater loss of membrane integrity when compared to their Fluconazole counterparts, but this effect was less pronounced than the membrane damage caused by Amphotericin B. The extract also made the strains more susceptible to Congo red and Calcofluor white. A synergistic action of the extract with Fluconazole and Micafungin was observed. The E. uniflora extract may be a viable option for the treatment of Candida infections.
有限的抗真菌药物库促使人们寻找具有生物活性的新型分子。本研究旨在表征茵芋提取物的抗真菌作用机制及其与市售抗真菌药物对以下念珠菌属物种的协同活性:白色念珠菌、热带念珠菌、光滑念珠菌、近平滑念珠菌和都柏林念珠菌。进行了计算机模拟分析,以预测提取物中主要化合物的抗真菌活性。在存在外源性麦角固醇和山梨醇的情况下测定最小抑菌浓度(MIC)。在应激条件下培养酵母细胞。使用碘化丙啶染色(荧光发射)评估细胞膜完整性的丧失。测定提取物与抗真菌化合物之间的协同作用(除时间杀伤曲线外)。分子对接显示了杨梅素和鞣花酸与参与麦角固醇和细胞壁生物合成的酶之间可能的相互作用。在添加外源性麦角固醇和山梨醇的情况下,用提取物培养的念珠菌细胞的 MIC 值增加了 2 至 8 倍。与氟康唑相比,用提取物处理的菌株显示出更大的细胞膜完整性丧失,但这种效应不如两性霉素 B 引起的膜损伤明显。提取物还使菌株对刚果红和Calcofluor 白更敏感。观察到提取物与氟康唑和米卡芬净的协同作用。茵芋提取物可能是治疗念珠菌感染的一种可行选择。