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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 35, Number 9
BKCSDE 35(9)
September 20, 2014 

Enhancement of Antibacterial Activity of Short Tryptophan-rich Antimicrobial Peptide Pac-525 by Replacing Trp with His(chx)
Mija Ahn, Ganesan Rajasekaran, Gunasekaran P, Eun kyoung Ryu, Ga-hyang Lee, Jae-Kyung Hyun, Chaejoon Cheong, Nam-Hyung Kim, Song Yub Shin*, Jeong-Kyu Bang*
Antimicrobial peptides, MRSA activity, Pac- 525, Light sensitivity, Short Trp-rich peptide
Trp residue is considered as one of the important constituents in antimicrobial peptides (AMPs) as it presence secured good activities in many cases. However, it is preferable to be changed because of their sensitivity towards light. We have synthesized the short Trp-rich AMP Pac-525 and its analogues to investigate the possibility of His(chx) as possible replacement analogue for Trp in AMPs. Based on the assay result of the antibacterial activity including anti-MRSA activity, His(chx) is considered as good candidate for the Trp replacement. Through these study, we found that His(chx) had several merits to design therapeutic antimicrobial agents compare to Trp in terms of i) increasing antibacterial activity without hemolytic activity, ii) successful in designing the short peptide (only four residues), iii) having anti-MRSA activity, iv) overcoming the light sensitivity. Furthermore, transmission electron microscopy (TEM) and dye leakage experiments suggested that P11 and P16 containing His(chx) kill bacteria via forming pore/ion channels on bacterial cell membranes.
2818 - 2824
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