Antimicrobial activity profiles of Amphiphilic Xanthone derivatives are a function of their molecular Oligomerization

Biochimica Et Biophysica Acta. Biomembranes
Jun-Jie KohShouping Liu

Abstract

Currently, membrane-targeting small antimicrobial peptidomimetics (SAP) are important in antibiotic development because bacteria appear to develop resistance to these surface-active compounds less readily. However, the molecular membrane-targeting action of SAPs has received little attention. In this study, we investigated the effect of oligomerization of amphiphilic xanthone, a model SAP, on its antimicrobial properties against both Gram-positive and Gram-negative bacteria. First, oligomer formation by an amphiphilic xanthone, compound 2 (also coded as AM052), was investigated via solution-state nuclear magnetic resonance (NMR) spectroscopy. Then, the effects of oligomerization on membrane disruption were further studied via biophysical approaches. The results showed that the antimicrobial activities of SAPs develop in several stages: oligomer formation in aqueous solution, initial binding of oligomers to the membrane-water interface followed by insertion into the membrane bilayer, aggregation of antimicrobial oligomers in the membrane, and induced membrane leakage. Ultimately, the presence of the oligomers in the bacterial membrane leads to decreased membrane fluidity and bacterial cell death. Interestingly, the early formati...Continue Reading

Citations

Mar 1, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Carla FernandesMadalena M M Pinto
Jan 19, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Joana AraújoMaria Elizabeth Tiritan
Sep 29, 2020·Chemistry : a European Journal·Alexandra ShchukinaKrzysztof Kazimierczuk
Mar 20, 2021·ACS Medicinal Chemistry Letters·Andrew J TagueStephen G Pyne
Apr 24, 2021·Nanoscale·Pingfan WuZicheng Xiao

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