High Antibacterial Activity and Selectivity of Cationic Disubstituted Polypeptoids with Stable Helices and Enzymatic Resistance DOI

Anyao Ma,

Xuehua Deng,

Lüxin Wei

et al.

ACS Applied Materials & Interfaces, Journal Year: 2025, Volume and Issue: unknown

Published: May 1, 2025

High antibacterial activity, low mammalian cell toxicity, and serum stability are crucial parameters for designing efficient materials under physiological conditions. This relies on a deep understanding of the structure-property relationship materials. In this study, series cationic amphiphilic disubstituted polypeptoids were synthesized by using ring-opening polymerization (ROP) followed thiol-ene click reactions. new class peptidomimetic materials, with chiral centers at backbones ammonium alkyl N-substituents, exhibited remarkably stable helical structures independent pH, temperature, salt, denaturing agents. The analogs found to show higher activity against both Gram-negative Gram-positive strains than racemic, nonhelical counterparts. structure balance charges hydrophobicity key achieve high selectivity bacteria over cells. Moreover, unlike poly(l-lysine), polypeptoids, helices enzymatic resistance, retained even in presence salts, human albumin (HSA), protease trypsin concentrations. study deepens our how structural elements correlate selectivity. addition, enzymatically have shown promise as an attractive platform design efficiency toxicity.

Language: Английский

High Antibacterial Activity and Selectivity of Cationic Disubstituted Polypeptoids with Stable Helices and Enzymatic Resistance DOI

Anyao Ma,

Xuehua Deng,

Lüxin Wei

et al.

ACS Applied Materials & Interfaces, Journal Year: 2025, Volume and Issue: unknown

Published: May 1, 2025

High antibacterial activity, low mammalian cell toxicity, and serum stability are crucial parameters for designing efficient materials under physiological conditions. This relies on a deep understanding of the structure-property relationship materials. In this study, series cationic amphiphilic disubstituted polypeptoids were synthesized by using ring-opening polymerization (ROP) followed thiol-ene click reactions. new class peptidomimetic materials, with chiral centers at backbones ammonium alkyl N-substituents, exhibited remarkably stable helical structures independent pH, temperature, salt, denaturing agents. The analogs found to show higher activity against both Gram-negative Gram-positive strains than racemic, nonhelical counterparts. structure balance charges hydrophobicity key achieve high selectivity bacteria over cells. Moreover, unlike poly(l-lysine), polypeptoids, helices enzymatic resistance, retained even in presence salts, human albumin (HSA), protease trypsin concentrations. study deepens our how structural elements correlate selectivity. addition, enzymatically have shown promise as an attractive platform design efficiency toxicity.

Language: Английский

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