{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,15]],"date-time":"2026-05-15T15:08:33Z","timestamp":1778857713894,"version":"3.51.4"},"reference-count":32,"publisher":"MDPI AG","issue":"8","license":[{"start":{"date-parts":[[2022,8,13]],"date-time":"2022-08-13T00:00:00Z","timestamp":1660348800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100012190","name":"Ministry of Science and Higher Education of the Russian Federation","doi-asserted-by":"publisher","award":["075-15-2021-1049"],"award-info":[{"award-number":["075-15-2021-1049"]}],"id":[{"id":"10.13039\/501100012190","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Marine Drugs"],"abstract":"<jats:p>In recent years, new antibiotics targeting multidrug resistant Gram-negative bacteria have become urgently needed. Therefore, antimicrobial peptides are considered to be a novel perspective class of antibacterial agents. In this study, a panel of novel BRICHOS-related \u03b2-hairpin antimicrobial peptides were identified in transcriptomes of marine polychaeta species. Two of them\u2014abarenicin from Abarenicola pacifica and UuBRI-21 from Urechis unicinctus\u2014possess strong antibacterial potential in vitro against a wide panel of Gram-negative bacteria including drug-resistant strains. Mechanism of action assays demonstrate that peptides disrupt bacterial and mammalian membrane integrity. Considering the stronger antibacterial potential and a low ability of abarenicin to be bound by components of serum, this peptide was selected for further modification. We conducted an alanine and arginine scanning of abarenicin by replacing individual amino acids and modulating hydrophobicity so as to improve its antibacterial potency and membrane selectivity. This design approach allowed us to obtain the Ap9 analog displaying a high efficacy in vivo in the mice septicemia and neutropenic mice peritonitis models. We demonstrated that abarenicin analogs did not significantly induce bacterial resistance after a four-week selection experiment and acted on different steps of the biofilm formation: (a) killing bacteria at their planktonic stage and preventing biofilm formation and (b) degrading pre-formed biofilm and killing embedded bacteria. The potent antibacterial and antibiofilm activity of the abarenicin analog Ap9 with its high efficacy in vivo against Gram-negative infection in mice models makes this peptide an attractive candidate for further preclinical investigation.<\/jats:p>","DOI":"10.3390\/md20080517","type":"journal-article","created":{"date-parts":[[2022,8,15]],"date-time":"2022-08-15T03:33:20Z","timestamp":1660534400000},"page":"517","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":21,"title":["Novel \u03b2-Hairpin Peptide from Marine Polychaeta with a High Efficacy against Gram-Negative Pathogens"],"prefix":"10.3390","volume":"20","author":[{"given":"Victoria N.","family":"Safronova","sequence":"first","affiliation":[{"name":"M. M. Shemyakin & Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, The Russian Academy of Sciences, Miklukho-Maklaya Str., 16\/10, 117997 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ilia A.","family":"Bolosov","sequence":"additional","affiliation":[{"name":"M. M. Shemyakin & Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, The Russian Academy of Sciences, Miklukho-Maklaya Str., 16\/10, 117997 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Roman N.","family":"Kruglikov","sequence":"additional","affiliation":[{"name":"M. M. Shemyakin & Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, The Russian Academy of Sciences, Miklukho-Maklaya Str., 16\/10, 117997 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Olga V.","family":"Korobova","sequence":"additional","affiliation":[{"name":"State Research Center for Applied Microbiology & Biotechnology (SRCAMB), 142279 Obolensk, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Eugenia S.","family":"Pereskokova","sequence":"additional","affiliation":[{"name":"State Research Center for Applied Microbiology & Biotechnology (SRCAMB), 142279 Obolensk, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6309-7645","authenticated-orcid":false,"given":"Alexander I.","family":"Borzilov","sequence":"additional","affiliation":[{"name":"State Research Center for Applied Microbiology & Biotechnology (SRCAMB), 142279 Obolensk, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8448-031X","authenticated-orcid":false,"given":"Pavel V.","family":"Panteleev","sequence":"additional","affiliation":[{"name":"M. M. Shemyakin & Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, The Russian Academy of Sciences, Miklukho-Maklaya Str., 16\/10, 117997 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5950-249X","authenticated-orcid":false,"given":"Tatiana V.","family":"Ovchinnikova","sequence":"additional","affiliation":[{"name":"M. M. Shemyakin & Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, The Russian Academy of Sciences, Miklukho-Maklaya Str., 16\/10, 117997 Moscow, Russia"},{"name":"Department of Bioorganic Chemistry, Faculty of Biology, Lomonosov Moscow State University, 119234 Moscow, Russia"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,8,13]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"457","DOI":"10.1016\/j.jgar.2020.02.030","article-title":"Prevalence of Multidrug-Resistant Gram-Negative Bacteria Cases at Admission in a Multispeciality Hospital","volume":"22","author":"Nagvekar","year":"2020","journal-title":"J. Glob. Antimicrob. Resist."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"194","DOI":"10.3389\/fcimb.2016.00194","article-title":"Antimicrobial Peptides: An Emerging Category of Therapeutic Agents","volume":"6","author":"Mahlapuu","year":"2016","journal-title":"Front. Cell. Infect. 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