Department of Cell Biology, Institute of Biology and Biochemistry, Maria Curie-Skłodowska University, 20-033 Lublin, Poland.
Eur J Pharm Sci. 2013 Aug 16;49(5):850-7. doi: 10.1016/j.ejps.2013.06.007. Epub 2013 Jun 19.
Amphotericin B (AmB) is a polyene antibiotic produced by Streptomyces nodosus used for more than 50 years in the treatment of acute systemic fungal infections. It exhibits a broad spectrum of activity against fungal and protozoan pathogens with relatively rare resistance. The aim of this study was to prepare and evaluate the utility of the AmB-Cu(2+) complex as a potential compound with a high fungicidal activity at lower concentrations, compared with conventional AmB. It was hypothesized that insertion of copper ions into fungal cell membranes, together with the AmB-Cu(2+) complex bypassing the natural homeostatic mechanisms of this element, may contribute to the increased fungicidal activity of AmB. The analysis of results indicates the increased antifungal activity of the AmB-Cu(2+) complex against Candida albicans in comparison with the pure AmB and Fungizone. Additionally, it was stated that the increased antifungal activity of the AmB-Cu(2+) complex is not the sum of the toxic effects of AmB and Cu(2+) ions, but is a result of the unique structure of this compound.
两性霉素 B（AmB）是一种由棘孢小单孢菌产生的多烯抗生素，用于治疗急性系统性真菌感染已有 50 多年的历史。它对真菌和原生动物病原体具有广泛的活性，耐药性相对较少。本研究旨在制备和评估 AmB-Cu(2+) 配合物的实用性，作为一种潜在的化合物，与传统的 AmB 相比，在较低浓度下具有更高的杀菌活性。假设铜离子插入真菌细胞膜，以及 AmB-Cu(2+) 配合物绕过该元素的自然动态平衡机制，可能有助于提高 AmB 的杀菌活性。结果分析表明，与纯 AmB 和 Fungizone 相比，AmB-Cu(2+) 配合物对白色念珠菌的抗真菌活性增加。此外，还指出 AmB-Cu(2+) 配合物的抗真菌活性不是 AmB 和 Cu(2+) 离子的毒性作用的总和，而是这种化合物独特结构的结果。
