Synthesis of cyclotetrapeptide analogues of c-PLAI and evaluation of their antimicrobial properties
Antimicrobial peptides (AMPs) are interesting compounds owing to their ability to kill several pathogens. In order to identify new AMPs, c-PLAI analogues were synthesized and evaluated together with their linear precursors for their antimicrobial properties against two Gram-positive bacteria (Staphy...
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The Royal Society
2021-03-01
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Series: | Royal Society Open Science |
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Online Access: | https://royalsocietypublishing.org/doi/pdf/10.1098/rsos.201822 |
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author | Rani Maharani Orin Inggriani Napitupulu Jelang M. Dirgantara Ace Tatang Hidayat Dadan Sumiarsa Desi Harneti Nurlelasari Unang Supratman Koichi Fukase |
author_facet | Rani Maharani Orin Inggriani Napitupulu Jelang M. Dirgantara Ace Tatang Hidayat Dadan Sumiarsa Desi Harneti Nurlelasari Unang Supratman Koichi Fukase |
author_sort | Rani Maharani |
collection | DOAJ |
description | Antimicrobial peptides (AMPs) are interesting compounds owing to their ability to kill several pathogens. In order to identify new AMPs, c-PLAI analogues were synthesized and evaluated together with their linear precursors for their antimicrobial properties against two Gram-positive bacteria (Staphylococcus aureus and Bacillus cereus), two Gram-negative bacteria (Escherichia coli and Klebsiella pneumoniae), and two fungal strains (Candida albicans and Trichophyton mentagrophytes). The new c-PLAI analogues were prepared through a combination of solid- and solution-phase syntheses, as previously employed for the synthesis of c-PLAI. The antimicrobial activity tests showed that the synthetic parent peptide c-PLAI was inactive or weakly active towards the bioindicators employed in the assay. The tests also indicated that cyclic c-PLAI analogues possessed enhanced antimicrobial properties against most of the bacteria and fungi tested. Furthermore, this study revealed that analogues containing cationic lysine residues displayed the highest activity towards most bioindicators. A combination of lysine and aromatic residues yielded analogues with broad-spectrum antimicrobial properties. |
first_indexed | 2024-12-22T12:17:15Z |
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id | doaj.art-56e53e1e87db490fb74f34c58541dae4 |
institution | Directory Open Access Journal |
issn | 2054-5703 |
language | English |
last_indexed | 2024-12-22T12:17:15Z |
publishDate | 2021-03-01 |
publisher | The Royal Society |
record_format | Article |
series | Royal Society Open Science |
spelling | doaj.art-56e53e1e87db490fb74f34c58541dae42022-12-21T18:26:06ZengThe Royal SocietyRoyal Society Open Science2054-57032021-03-018310.1098/rsos.201822201822Synthesis of cyclotetrapeptide analogues of c-PLAI and evaluation of their antimicrobial propertiesRani MaharaniOrin Inggriani NapitupuluJelang M. DirgantaraAce Tatang HidayatDadan SumiarsaDesi HarnetiNurlelasariUnang SupratmanKoichi FukaseAntimicrobial peptides (AMPs) are interesting compounds owing to their ability to kill several pathogens. In order to identify new AMPs, c-PLAI analogues were synthesized and evaluated together with their linear precursors for their antimicrobial properties against two Gram-positive bacteria (Staphylococcus aureus and Bacillus cereus), two Gram-negative bacteria (Escherichia coli and Klebsiella pneumoniae), and two fungal strains (Candida albicans and Trichophyton mentagrophytes). The new c-PLAI analogues were prepared through a combination of solid- and solution-phase syntheses, as previously employed for the synthesis of c-PLAI. The antimicrobial activity tests showed that the synthetic parent peptide c-PLAI was inactive or weakly active towards the bioindicators employed in the assay. The tests also indicated that cyclic c-PLAI analogues possessed enhanced antimicrobial properties against most of the bacteria and fungi tested. Furthermore, this study revealed that analogues containing cationic lysine residues displayed the highest activity towards most bioindicators. A combination of lysine and aromatic residues yielded analogues with broad-spectrum antimicrobial properties.https://royalsocietypublishing.org/doi/pdf/10.1098/rsos.201822c-plaicyclotetrapeptideantimicrobial peptidesolid-phase peptide synthesis |
spellingShingle | Rani Maharani Orin Inggriani Napitupulu Jelang M. Dirgantara Ace Tatang Hidayat Dadan Sumiarsa Desi Harneti Nurlelasari Unang Supratman Koichi Fukase Synthesis of cyclotetrapeptide analogues of c-PLAI and evaluation of their antimicrobial properties Royal Society Open Science c-plai cyclotetrapeptide antimicrobial peptide solid-phase peptide synthesis |
title | Synthesis of cyclotetrapeptide analogues of c-PLAI and evaluation of their antimicrobial properties |
title_full | Synthesis of cyclotetrapeptide analogues of c-PLAI and evaluation of their antimicrobial properties |
title_fullStr | Synthesis of cyclotetrapeptide analogues of c-PLAI and evaluation of their antimicrobial properties |
title_full_unstemmed | Synthesis of cyclotetrapeptide analogues of c-PLAI and evaluation of their antimicrobial properties |
title_short | Synthesis of cyclotetrapeptide analogues of c-PLAI and evaluation of their antimicrobial properties |
title_sort | synthesis of cyclotetrapeptide analogues of c plai and evaluation of their antimicrobial properties |
topic | c-plai cyclotetrapeptide antimicrobial peptide solid-phase peptide synthesis |
url | https://royalsocietypublishing.org/doi/pdf/10.1098/rsos.201822 |
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