Antibacterial, antifungal activities and toxicity of new synthetic fatty acid salicylate esters
作者:Monique B. Ewonkem、Pascaline M. Deussom、Michel A. Mbock、Eunice N. Tiakouang、Alfred F. A. Toze、Duplex J. Wansi
DOI:10.1007/s00044-023-03034-w
日期:2023.4
myristic) and unsaturated long-chain (oleic, linoleic, eleostearic) fatty acid units quenched the antimicrobial activity. Also, esterifying the phenolic OH and increasing the number of benzene ring reduced, on one hand the antibacterial activity of the compounds bearing the palmitic acid and, on the other, increased their antifungal activity. Acute toxicity experiments revealed that mono salicyl-palmitate is
微生物威胁及其对现有药物的耐药性是全球科学家正在努力解决的公共卫生问题。在发现传统药物之前,脂肪酸和水杨酸衍生物等天然产物已显示出对抗病原体的功效,如今,它们被认为是下一代抗菌剂。本研究旨在制备新型抗菌抗真菌药物,以脂肪酸和水杨酸盐衍生物为原料,设计合成了24种新型水杨酸盐-脂肪酸,并在多种细菌和真菌菌株上进行了体外试验。结果发现,与棕榈酸共价连接的水杨酸盐具有良好(MIC = 31.25 μg/ml)和中等(MIC = 62.5 和 125 μg/ml)抗菌和抗真菌活性肺炎链球菌、金黄色葡萄球菌、伤寒杆菌、肺炎克雷伯菌、大肠杆菌、须癣毛癣菌、奥杜氏小孢子菌、絮状表皮癣菌和石膏小孢子菌. 据观察,饱和中链(月桂酸、肉豆蔻酸)和不饱和长链(油酸、亚油酸、桐酸)脂肪酸单元会抑制抗菌活性。此外,酯化酚羟基和增加苯环数量一方面降低了带有棕榈酸的化合物的抗菌活性,另一方面增加了它们的抗真菌活性。急性