1 research outputs found
Conjugation of Polyphosphoester and Antimicrobial Peptide for Enhanced Bactericidal Activity and Biocompatibility
Enhancing the bactericidal activity and moderating the toxicity
are two important challenges in the design of upcoming antimicrobial
compounds. Herein, antimicrobial macromolecules were developed by
conjugating CysHHC10 peptide and polyphosphoester for the modulation
of microbiocidal activity and biocompatibility. The conjugation was
carried out via thiol-yne “click” chemistry between
the cysteine terminal of the peptide and the pendant propargyl moieties
of the polyphosphoester. The bactericidal efficacy of the polyphosphoester–peptide
conjugates were investigated by microbial growth inhibition toward
the Gram-positive and Gram-negative bacteria. On the basis of peptide
mass fraction, the polyphosphoester–peptide conjugates exhibited
lower values of minimum inhibitory concentration than that of the
free peptide. The polyphosphoester–peptide conjugates also
exhibited ultralow hemolytic characteristic at a concentration of
4000 μg/mL, indicating significant improvement of erythrocytes
compatibility as compared to the free peptide that readily caused
lysis of 50% of red blood cells at 1000 μg/mL. Cytotoxicity
of the polyphosphoester–peptide conjugates toward 3T3 fibroblast
cells was also reduced in comparison to that of the free peptide.
Conjugation of the polyphosphoester thus improves the bactericidal
efficacy and biocompatibility of the antimicrobial peptide