OBJECTIVE: To construct antimicrobial peptides with potent antimicrobial activity, low cytotoxicity and efficient killing rate of for prevention and treatment of dental caries. METHODS: We exploited the existing design strategies to modify reutericin 6 or gassericin A produced by species in the oral cavity based on their cationicity, amphipathicity and -helical structure. We examined their antimicrobial activities using bacterial susceptibility assay, their cytotoxicity through cytotoxicity assay and their killing rate of with time-kill assay. We further evaluated the candidate derivatives for their killing rate against , their antimicrobial activity against different oral pathogens and the development of drug resistance. RESULTS: We constructed 6 AT-1 derivatives, among which AT-7 showed an MIC of 3.3 μmol/L against , and with a killing rate of 88.7% against within 5 min. We did not obtain strains of resistant to AT- 7 after induction for 10 passages. CONCLUSIONS Hydrophobicity and imperfect amphipathic structure are two key parameters that define the antimicrobial potency of the antimicrobial peptides. The imperfectly amphipathic peptide AT-7 shows the potential for clinical application in dental caries treatment.
Anti-Infective Agents ; Dental Caries ; Humans ; Microbial Sensitivity Tests ; Peptides ; Streptococcus mutans