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Mar. Drugs 2018, 16(12), 466;

Cytotoxic Potential of the Novel Horseshoe Crab Peptide Polyphemusin III

M.M. Shemyakin & Yu.A. Ovchinnikov Institute of Bioorganic Chemistry, the Russian Academy of Sciences, Mikhluho-Maklaya str. 16/10, Moscow 117997, Russia
Department of Bioinformatics and Molecular Networks, Omicsway Corp., Walnut, CA 91789, USA
Department of Biotechnology, I.M. Sechenov First Moscow State Medical University (Sechenov University), Moscow 119991, Russia
Author to whom correspondence should be addressed.
Received: 3 November 2018 / Revised: 19 November 2018 / Accepted: 20 November 2018 / Published: 26 November 2018
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Biological activity of the new antimicrobial peptide polyphemusin III from the horseshoe crab Limulus polyphemus was examined against bacterial strains and human cancer, transformed, and normal cell cultures. Polyphemusin III has the amino acid sequence RRGCFRVCYRGFCFQRCR and is homologous to other β-hairpin peptides from the horseshoe crab. Antimicrobial activity of the peptide was evaluated and MIC (minimal inhibitory concentration) values were determined. IC50 (half-maximal inhibitory concentration) values measured toward human cells revealed that polyphemusin III showed a potent cytotoxic activity at concentrations of <10 μM. Polyphemusin III caused fast permeabilization of the cytoplasmic membrane of human leukemia cells HL-60, which was measured with trypan blue exclusion assay and lactate dehydrogenase-release assay. Flow cytometry experiments for annexin V-FITC/ propidium iodide double staining revealed that the caspase inhibitor, Z-VAD-FMK, did not abrogate disruption of the plasma membrane by polyphemusin III. Our data suggest that polyphemusin III disrupts the plasma membrane integrity and induces cell death that is apparently not related to apoptosis. In comparison to known polyphemusins and tachyplesins, polyphemusin III demonstrates a similar or lower antimicrobial effect, but significantly higher cytotoxicity against human cancer and transformed cells in vitro. View Full-Text
Keywords: antimicrobial peptide; cytotoxicity; β-hairpin; polyphemusins; tachyplesins; cell death; signaling pathways antimicrobial peptide; cytotoxicity; β-hairpin; polyphemusins; tachyplesins; cell death; signaling pathways

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Marggraf, M.B.; Panteleev, P.V.; Emelianova, A.A.; Sorokin, M.I.; Bolosov, I.A.; Buzdin, A.A.; Kuzmin, D.V.; Ovchinnikova, T.V. Cytotoxic Potential of the Novel Horseshoe Crab Peptide Polyphemusin III. Mar. Drugs 2018, 16, 466.

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