Department of Food, Environmental and Nutritional Sciences (DeFENS), University of Milan, Via Celoria 2, 20133 Milan, Italy.
Molecular Pharmacology Unit, Department of Applied Research and Technological Development, Fondazione IRCCS Istituto Nazionale Tumori, Via Amadeo 42, 20133 Milan, Italy.
Int J Mol Sci. 2020 Mar 21;21(6):2168. doi: 10.3390/ijms21062168.
In a recent study, we investigated the antimicrobial activity of a collection of resveratrol-derived monomers and dimers against a series of foodborne pathogens. Out of the tested molecules, dehydro--viniferin and dehydro--viniferin emerged as the most promising derivatives. To define the structural elements essential to the antimicrobial activity against the foodborne pathogen Scott A as a model Gram-positive microorganism, the synthesis of a series of simplified benzofuran-containing derivatives was carried out. The systematic removal of the aromatic moieties of the parent molecules allowed a deeper insight into the most relevant structural features affecting the activity. While the overall structure of compound could not be altered without a substantial loss of antimicrobial activity, the structural simplification of compound (minimal inhibitory concentration (MIC) 16 µg/mL, minimal bactericidal concentration (MBC) >512 µg/mL) led to the analogue with increased activity (MIC 8 µg/mL, MBC 64 µg/mL).
在最近的一项研究中，我们研究了一组白藜芦醇衍生的单体和二聚体对一系列食源性病原体的抗菌活性。在测试的分子中，脱氢白藜芦醇和脱氢白藜芦醇二聚体脱颖而出，成为最有前途的衍生物。为了确定对食源性病原体 Scott A 的抗菌活性至关重要的结构元素，我们以革兰氏阳性微生物为模型，合成了一系列简化的含苯并呋喃的衍生物。系统地去除母体分子的芳基部分可以更深入地了解影响活性的最相关结构特征。虽然化合物的整体结构不能改变，否则抗菌活性会大幅下降，但化合物的结构简化（最小抑菌浓度 (MIC) 为 16 μg/mL，最小杀菌浓度 (MBC) >512 μg/mL）导致类似物的活性增加（MIC 为 8 μg/mL，MBC 为 64 μg/mL）。
