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KMID : 0043320170400121414
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Archives of Pharmacal Research
2017 Volume.40 No. 12 p.1414 ~ p.1419
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Antimicrobial activity and stability of stapled helices of polybia-MP1
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Luong Huy X.
Kim Do-Hee
Lee Bong-Jin
Kim Young-Woo
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Abstract
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Polybia-MP1 is a well-known natural antimicrobial peptide isolated from the venom of the social wasp Polybia paulista. A recent study showed that this peptide displays a broad antibacterial spectrum as well as low toxicity to human red blood cells and normal fibroblasts. However, its moderate antimicrobial activity and high susceptibility to protease have been a major hurdle for clinical use. This study examined the possibility of developing biologically more potent, yet metabolically more stable, analogues of MP1 using an emerging technology termed “all-hydrocarbon stapling.” The stapled analogues of MP1 showed more than a threefold increase in helicity as well as an approximately 70-fold enhancement in proteolytic stability. These stapled analogues also exhibited a significant increase in inhibition against some Gram-positive bacteria while displaying a modest enhancement in hemolytic activity. Overall, the current study demonstrated that the all-hydrocarbon stapling system is a highly useful tool for the development of biologically more potent and metabolically more stable analogues of natural antimicrobial peptides.
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KEYWORD
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Antimicrobial peptides, α-Helix, Stapled peptides, Amphipathic peptides, Proteolytic resistance
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