Abstract
The natural antimicrobial peptide Polybia-MP1 is a promising candidate for develo** new treatment therapy for infection and cancer. It showed broad-spectrum antimicrobial and anticancer activity with high safety on healthy cells. However, previous sequence modification usually resulted in at least one of two consequences: a notable increase in hemolytic activity or a considerable decrease in activity against Gram-negative bacteria and cancer cells. Herein, a new approach was applied by replacing the amino acid Glutamine at position 12 with Lysine and generating the MP1-Q12K analog. Our preliminary data suggested an enhancement in antibacterial and antifungal activity, whereas the anticancer and hemolytic activity of the two peptides were comparable. Moreover, MP1-Q12K was found to be less self-assembly than Polybia-MP1, which further supports the enhancement of antimicrobial properties. Hence, this study provides new information regarding the structure–activity relationships of Polybia-MP1 and support for the development of potent, selective antimicrobial peptides.
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The data that support the findings of this study are openly available at https://doi.org/10.1007/s00726-023-03276-3.
Abbreviations
- AMP:
-
Antimicrobial peptide
- DMSO:
-
Dimethyl sulfoxide
- HPLC:
-
High performance liquid chromatography
- PC:
-
Phosphatidylcholine
- PE:
-
Phosphatidylethanolamines
- PS:
-
Phosphatidylserin
- RBC:
-
Red blood cell
- SARs:
-
Structure–activity relationships
- MP1:
-
Polybia-MP1
- MTT :
-
3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide
- SDS:
-
Sodium Dodecyl sulfate
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Acknowledgements
This research is funded by The PHENIKAA University Foundation for Science and Technology Development, Grant number 2-01.2020.02.
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The PHENIKAA University Foundation for Science and Technology Development, Grant number 2-01.2020.02.
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H.B.T.P., H.T.T. and H.L.X wrote the manuscript text, H.B.T.P. and H.L.X prepared Figures 1, 2, 5 and 6. H.T.T prepared Figure 3. H.B.T.P, H.P.T and M.N.H prepared Table 2 and Table 3. H.P.T and M.C.V prepared Figure 4. H.B.T.P, V.A.T, K.N.N and V.N.H synthesized peptides. All authors reviewed the manuscript.
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Phuong, H.B.T., Tran, V.A., Ngoc, K.N. et al. Effect of substituting glutamine with lysine on structural and biological properties of antimicrobial peptide Polybia-MP1. Amino Acids 55, 881–890 (2023). https://doi.org/10.1007/s00726-023-03276-3
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DOI: https://doi.org/10.1007/s00726-023-03276-3