4.5 Article

Novel tetrameric cell penetrating antimicrobial peptoids effective against mycobacteria and drug-resistant Staphylococcus aureus

期刊

FRONTIERS IN BIOSCIENCE-LANDMARK
卷 27, 期 2, 页码 -

出版社

IMR PRESS
DOI: 10.31083/j.fbl2702064

关键词

peptoids; antimicrobial; cell penetrating; MRSA; Mycobacterium tuberculosis

资金

  1. Deutsche Forschungsgemeinschaft (DFG), within the Research Training Group 2039
  2. Helmholtz Program Biointerfaces in Techology and Medicine (BIF-TM)
  3. Deutsche Forschungs-gemeinschaft (DFG, German Research Foundation) under Germany's Excellence Strategy via the Excellence Cluster 3D Matter Made to Order [EXC-2082/1 - 390761711]
  4. Singapore Ministry of Health's National Medical Research Council under its Individual Research Grant Scheme [NMRC/OFIRG/0026/2016]

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This study found that short tetrameric peptoids composed of a balance of aromatic and lipophilic residues have potent selective antimicrobial activity against various microorganisms, including drug-resistant Staphylococcus aureus and mycobacteria. These peptoids also demonstrated cell-penetrating capabilities in HeLa and RAW 264.7 macrophage cells.
Background: Antimicrobial peptides (AMPs) are short, cationic, amphipathic molecules that have gained tremendous popularity as alternatives to traditional antibiotics due to their lower propensity to develop bacterial resistance. However, the clinical developability of AMPs remains impeded due to shortcomings such as proteolytic instability and poor penetration leading to low bioavailability. Aims: To improve the access of AMPs to cells and subsequent bacteria killing, we evaluated the cell-penetrating and antimicrobial properties of three novel libraries of synthetic peptoids using Minimum Inhibitory Concentration, killing efficacy and membrane permeabilization assays against mycobacteria and Staphylococcus aureus. In addition, we investigated cell selectivity using mammalian cells to assess peptoid toxicity. Results: We showed that short tetrameric Rhodamine B-labeled peptoids composed of a balance of aromatic and lipophilic residues have potent selective antimicrobial activity against a range of microorganisms. The most potent candidates were active against drug-resistant S. aureus isolates as well as mycobacterial strains, with cell penetrating capabilities reported in HeLa and RAW 264.7 macrophage cells. Conclusions: These data suggest that peptoids with novel dual functionalities may potentially be an interesting class of therapeutics and/or molecular delivery agents for anti-infective purposes.

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