Nałęcz-Jawecki Grzegorz, Wawryniuk Milena, Kopczyńska Weronika, Giebułtowicz Joanna
Department of Toxicology and Food Science, Medical University of Warsaw, 02-091 Warszawa, Poland.
Department of Drug Chemistry, Pharmaceutical and Biomedical Analysis, Medical University of Warsaw, 02-091 Warszawa, Poland.
Molecules. 2025 Apr 25;30(9):1907. doi: 10.3390/molecules30091907.
Co-trimoxazole is an antibacterial drug, a mixture of sulfamethoxazole (SMX) and trimethoprim (TMP) in a ratio of 5:1. Due to the different susceptibility of both components to decomposition under the influence of sunlight, the aim of the study was to assess the change in bacteriostatic activity during irradiation of the mixture of these antibiotics in a sunlight simulator. The bacteriostatic activity was assessed using a Microbial Assay for Risk Assessment (MARA), monitoring drug concentrations as well as the formation of photodegradation products using liquid chromatography (LC). The toxicity analysis of the SMX and TMP mixture showed synergistic bacteriostatic activity for six bacterial strains. This activity was maintained even during sample irradiation when 80-90% of SMX was degraded. This may indicate the bacteriostatic effect of SMX photoproducts and/or the lack of necessity to maintain a 5:1 ratio between SMX and TMP to maintain a strong effect of the mixture of these antibiotics. Analysis using LC with a high-resolution mass spectrometry detector revealed the presence of 11 SMX degradation products, including two with preserved sulfonamide structure, which may exhibit bacteriostatic activity.
复方新诺明是一种抗菌药物,是磺胺甲恶唑(SMX)和甲氧苄啶(TMP)按5:1比例混合而成的。由于两种成分在阳光照射下分解的敏感性不同,本研究的目的是评估在阳光模拟器中照射这些抗生素混合物期间抑菌活性的变化。使用风险评估微生物测定法(MARA)评估抑菌活性,通过液相色谱法(LC)监测药物浓度以及光降解产物的形成。SMX和TMP混合物的毒性分析表明,对六种细菌菌株具有协同抑菌活性。即使在80-90%的SMX降解的样品照射期间,这种活性也能维持。这可能表明SMX光产物的抑菌作用和/或维持SMX与TMP之间5:1的比例以保持这些抗生素混合物的强效作用并非必要。使用配备高分辨率质谱检测器的LC分析发现存在11种SMX降解产物,其中两种具有保留的磺酰胺结构,可能具有抑菌活性。