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ï¿½D1. Current and new peptide mimicking structures.

ï¿½D2. (A) Synthesis of HDP mimetics Gly-POX_n. (B) GPC traces of representative N-Boc protected Gly-POX_n. (C) MIC values of the Gly-POX_n with variable chain length against S. aureus using representative HDP magainin II as the control. (D) The MIC and MBC values of Gly-POX₂₀ against S. aureus (S.a), S. epidermis (S.e) and B. nsubtilis (B.sub). (E) Antimicrobial resistance test on Gly-POX₂₀ and Norfloxacin against S. aureus ATCC6538. (F) The change of MBC in antibiotics against Gly-POX₂₀ and norfloxacin treated S. aureus. S.a-Gly-POX₂₀-P928 was the S. aureus obtained after being treated with POX₂₀ continuously at 0.5×MBC concentration for 928 generations. S.a-Nor-P327 was the S.aureus obtained after being treated with norfloxacin continuously at 0.5×MBC concentration for 327 generations. (G) Killing kinetics of Gly-POX₂₀ at 4×MIC against MRSA persisters generated by 10×MIC ciprofloxacin treatment.

ï¿½D3. (A) Synthesis of morpholino-naphthalimide dye conjugated Gly-POX₂₀ (Dye-Gly-POX₂₀). (B) Time-laps fluorescent confocal imaging on the interaction between S. aureus and Dye-Gly-POX₂₀ (at 1×MBC) in the presence of propidium iodide. (C) Ortho view of Z-stack images on S. aureus after incubation with Dye-Gly-POX₂₀ (at 1×MBC) for 1260s. (D) Gly-POX₂₀-induced S. aureus cytoplasmic membrane depolarization assay. (E) The electrophoretic mobility shift assay of plasmid DNA and the mixture of plasmid DNA-complexes at different ratios of N:P (Gly-POX₂₀:DNA). (F) Intracellular ROS intensity produced by S. aureus in the presence of PBS, Gly-POX₂₀ (at 1×MBC), and the mixture of Gly-POX₂₀(1×MBC) and NAC (10 mM). ** p<0.01. (G) MBC value of Gly-POX₂₀ against S. aureus in the presence or absence of NAC (10 mM).

ï¿½D4. In vivo antibacterial efficacy study using a rat full-thickness wound model of MRSA infection. (A) Description of the in vivo infectious animal model using S. aureus USA300 LAC. (B) Cell density of S. aureus in infected tissues on day 1 after treatment with 250 MIC Gly-POX₂₀ and vancomycin (Van). ** p<0.01. (C) Infected wound photographs at defined time points showing representative result from 6 individual animals in each group. (D) Wound closure analysis expressed relative to the original size of the wound at day 0. Data are presented as the mean (n ï¿½ï¿½ 3 in each group). (E) Histological analysis on wound tissue sections stained with H&E on day 11 after antimicrobial treatment (blue arrow: inflammatory cells; green arrow: fibroblasts; yellow arrow: new collagen; orange arrow: new blood vessels; black arrow: calcareous clumps along with multicellular macrophages).

Õ“ï¿½ï¿½æœ½ï¿½: https://onlinelibrary.wiley.com/doi/abs/10.1002/ange.202000505

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