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Rational design of peptides with enhanced antimicrobial and anti‐biofilm activities against cariogenic bacterium Streptococcus mutans
Author(s) -
Liang Dongsheng,
Li Huanying,
Xu Xiaohu,
Liang Jingheng,
Dai Xingzhu,
Zhao Wanghong
Publication year - 2019
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13579
Subject(s) - streptococcus mutans , biofilm , antimicrobial , microbiology and biotechnology , chemistry , peptide , dental plaque , chlorhexidine , antimicrobial peptides , in vitro , bacteria , cytotoxicity , minimum inhibitory concentration , biology , biochemistry , medicine , dentistry , genetics
Streptococcus mutans ( S. mutans ) is known to be a leading cariogenic pathogen in the oral cavity. Antimicrobial peptides possess excellent properties to combat such pathogens. In this study, we compared the antimicrobial activity of novel linear reutericin 6‐ and/or gassericin A‐inspired peptides and identified LR ‐10 as the leading peptide. Antibacterial assays demonstrate that LR ‐10 is more active against S. mutans (3.3 μM) than many peptide‐based agents without resistance selection, capable of killing many oral pathogens, and tolerant of physiological conditions. LR ‐10 also presented a faster killing rate than chlorhexidine and erythromycin, and appeared to display selective activity against S. mutans within 10 s. S. mutans is usually encased in plaque biofilms. Biofilm inhibitory assays indicated that LR ‐10 had excellent inhibitory effect on the biofilm formation of S. mutans and biofilm‐encased cells in vitro at low concentrations (6.5 μM). Consistent with most peptides, LR ‐10 kills S. mutans mainly by disrupting the cell membranes. Notably, both hemolytic activity assays and cytotoxicity tests indicated that LR ‐10 could keep biocompatible at the effective concentrations. Hence, LR ‐10 could be a good candidate for clinical treatment of dental caries.