Rubio Cecilia, Ramírez Javiera, Weinstein-Oppenheimer Caroline, Bahamondez-Canas Tania F, Quiñones Natalia
Herbario de Líquenes, Escuela de Química y Farmacia, Facultad de Farmacia, Universidad de Valparaíso, Valparaíso 2340000, Chile.
Magíster en Gestión Farmacéutica y Farmacia Asistencial, Escuela de Química y Farmacia, Facultad de Farmacia, Universidad de Valparaíso, Valparaíso 2340000, Chile.
Molecules. 2025 Mar 18;30(6):1368. doi: 10.3390/molecules30061368.
Antimicrobial resistance is a global threat, highlighting the urgent need for novel antimicrobial agents. Among the mechanisms of resistance, bacteria can release drug-degrading enzymes and express efflux pumps, as well as grow in protected aggregates known as biofilms. and are among the most prevalent biofilm infections in chronic wounds, respiratory and urinary tract infections, and device-associated infections. (Delise) Malme is a lichen with metabolites with unexplored antimicrobial potential.
To identify and characterize the major metabolites present in and to determine their antimicrobial activity against and .
The molecules were purified by column chromatography and characterized by NMR spectroscopy. The antimicrobial activity of the compounds was determined in terms of proliferation, adhesion, and viability against and by the broth microdilution method and crystal violet staining. Viability was determined by the resazurin reduction assay on normal human fibroblasts to determine cytotoxicity over human cells.
The major metabolites were spectroscopically characterized and identified as physciosporin and methyl virensate. Physciosporin showed antimicrobial activity on with a MIC of 32 μg/mL and MBC of 128 μg/mL, and prevented biofilm formation from 16 μg/mL. Methyl virensate also had antimicrobial activity on (MIC = 64 μg/mL). None of these metabolites significantly affected proliferation, viability, or adhesion. Cytotoxicity of physciosporin at 16 ug/mL on normal human fibroblasts was below 20%.
This is the first report on the study of the antimicrobial activity of these compounds. Physciosporin showed promising activity in preventing the formation of biofilms, which are responsible for chronic infections. These findings provide a foundation for exploring the antimicrobial potential of other lichenic depsidones.
抗菌药物耐药性是一个全球性威胁,凸显了对新型抗菌药物的迫切需求。在耐药机制中,细菌可释放药物降解酶、表达外排泵,还能在被称为生物膜的受保护聚集体中生长。[具体细菌名称1]和[具体细菌名称2]是慢性伤口、呼吸道和泌尿道感染以及与器械相关感染中最常见的生物膜感染病原体。地衣(Delise)Malme含有具有未被探索的抗菌潜力的代谢产物。
鉴定并表征[地衣名称]中存在的主要代谢产物,并确定它们对[具体细菌名称1]和[具体细菌名称2]的抗菌活性。
通过柱色谱法纯化分子,并通过核磁共振光谱进行表征。采用肉汤微量稀释法和结晶紫染色法,根据化合物对[具体细菌名称1]和[具体细菌名称2]的增殖、黏附及活力来测定其抗菌活性。通过刃天青还原试验测定正常人类成纤维细胞的活力,以确定对人类细胞的细胞毒性。
主要代谢产物通过光谱表征并鉴定为扁枝衣菌素和甲基绿盘衣酸。扁枝衣菌素对[具体细菌名称1]显示出抗菌活性,最低抑菌浓度(MIC)为32μg/mL,最低杀菌浓度(MBC)为128μg/mL,且在16μg/mL时可阻止生物膜形成。甲基绿盘衣酸对[具体细菌名称1]也具有抗菌活性(MIC = 64μg/mL)。这些代谢产物均未显著影响[具体细菌名称2]的增殖、活力或黏附。16μg/mL的扁枝衣菌素对正常人类成纤维细胞的细胞毒性低于20%。
这是关于这些化合物抗菌活性研究的首次报道。扁枝衣菌素在预防导致慢性感染的[具体细菌名称1]生物膜形成方面显示出有前景的活性。这些发现为探索其他地衣缩酚酸类化合物的抗菌潜力奠定了基础。