English
norskBlar i forfatter "Blencke, Hans-Matti"
Viser treff 1-12 av 12
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Amphipathic Barbiturates as Mimics of Antimicrobial Peptides and the Marine Natural Products Eusynstyelamides with Activity against Multi-resistant Clinical Isolates
(Journal article; Tidsskriftartikkel; Peer reviewed, 2021-07-27)We report a series of synthetic cationic amphipathic barbiturates inspired by the pharmacophore model of small antimicrobial peptides (AMPs) and the marine antimicrobials eusynstyelamides. These N,N′-dialkylated-5,5-disubstituted barbiturates consist of an achiral barbiturate scaffold with two cationic groups and two lipophilic side chains. Minimum inhibitory concentrations of 2–8 μg/mL were achieved ... -
Anti-infectious and anti-inflammatory effects of peptide fragments sequentially derived from the antimicrobial peptide centrocin 1 isolated from the green sea urchin, Strongylocentrotus droebachiensis
(Journal article; Tidsskriftartikkel; Peer reviewed, 2012)Bacterial resistance against antibiotic treatment has become a major threat to public health. Antimicrobial peptides (AMPs) have emerged as promising alternative agents for treatment of infectious diseases. This study characterizes novel synthetic peptides sequentially derived from the AMP centrocin 1, isolated from the green sea urchin, for their applicability as anti-infective agents.The microbicidal ... -
The antimicrobial effect of CEN1HC-Br against Propionibacterium acnes and its therapeutic and anti-inflammatory effects on acne vulgaris
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-12-03)Propionibacterium acnes is a commensal bacterium, which is involved in acne inflammation. An antimicrobial peptide named CEN1HC-Br, which was isolated and characterized form the green sea urchin, has been shown to possess broad-spectrum antibacterial activity. Little is known concerning the potential effects of its antibacterial and anti-inflammatory properties against P. acnes. To examine the potency ... -
Antimicrobial peptides in echinoderm host defense
(Journal article; Tidsskriftartikkel; Peer reviewed, 2014-11-06)Antimicrobial peptides (AMPs) are important effector molecules in innate immunity. Here we briefly summarize characteristic traits of AMPs and their mechanisms of antimicrobial activity. Echinoderms live in a microbe-rich marine environment and are known to express a wide range of AMPs. We address two novel AMP families from coelomocytes of sea urchins: cysteine-rich AMPs (strongylocins) and ... -
A concise SAR-analysis of antimicrobial cationic amphipathic barbiturates for an improved activity-toxicity profile
(Journal article; Tidsskriftartikkel; Peer reviewed, 2022-08-05)An amphipathic barbiturate mimic of the marine eusynstyelamides is reported as a promising class of antimicrobial agents. We hereby report a detailed analysis of the structure-activity relationship for cationic amphipathic N,N′ -dialkylated-5,5-disubstituted barbiturates. The influence of various cationic groups, hydrocarbon linkers and lipophilic side chains on the compounds’ antimicrobial potency ... -
Expression of antimicrobial peptides in coelomocytes and embryos of the green sea urchin (Strongylocentrotus droebachiensis)
(Journal article; Tidsskriftartikkel; Peer reviewed, 2013-11-12)Antimicrobial peptides (AMPs) play a crucial role in innate immunity. We have previously reported the isolation and characterization of the AMPs, strongylocins 1 and 2, and centrocin 1, from coelomocyte extracts of Strongylocentrotus droebachiensis. Here we show that these AMPs were expressed in phagocytes. In addition, transcripts of strongylocin 1 were detected in vibratile cells and/or colorless ... -
Investigation of tetrasubstituted heterocycles reveals hydantoins as a promising scaffold for development of novel antimicrobials with membranolytic properties
(Journal article; Tidsskriftartikkel; Peer reviewed, 2023-01-24)Mimics of antimicrobial peptides (AMPs) have been proposed as a promising class of antimicrobial agents. We report the analysis of five tetrasubstituted, cationic, amphipathic heterocycles as potential AMP mimics. The analysis showed that the heterocyclic scaffold had a strong influence on the haemolytic activity of the compounds, and the hydantoin scaffold was identified as a promising template for ... -
Isolation and characterization of antimicrobial peptides with unusual disulfide connectivity from the colonial ascidian Synoicum turgens
(Journal article; Tidsskriftartikkel; Peer reviewed, 2020-01-12)This study reports the isolation of two novel cysteine-rich antibacterial peptides, turgencin A and turgencin B, along with their oxidized derivatives, from the Arctic marine colonial ascidian <i>Synoicum turgens</i>. The peptides are post-translationally modified, containing six cysteines with an unusual disulfide connectivity of Cys<sup>1</sup>-Cys<sup>6</sup>, Cys<sup>2</sup>-Cys<sup>5</sup>, and ... -
Isolation and Characterization of Antimicrobial Peptides with Unusual Disulfide Connectivity from the Colonial Ascidian Synoicum turgens
(Journal article; Tidsskriftartikkel; Peer reviewed, 2020-01-12)This study reports the isolation of two novel cysteine-rich antibacterial peptides, turgencin A and turgencin B, along with their oxidized derivatives, from the Arctic marine colonial ascidian <i>Synoicum turgens</i>. The peptides are post-translationally modified, containing six cysteines with an unusual disulfide connectivity of Cys<sup>1</i>-Cys<sup>6</sup>, Cys<sup>2</sup>-Cys<sup>5</sup>, and ... -
Outer Membrane Integrity-Dependent Fluorescence of the Japanese Eel UnaG Protein in Live Escherichia coli Cells
(Journal article; Tidsskriftartikkel; Peer reviewed, 2023-02-07)Reporter genes are important tools in many biological disciplines. The discovery of novel reporter genes is relatively rare. However, known reporter genes are constantly applied to novel applications. This study reports the performance of the bilirubin-dependent fluorescent protein UnaG from the Japanese eel Anguilla japonicas in live Escherichia coli cells in response to the disruption of outer ... -
Structure-activity relationships of the antimicrobial peptide arasin 1 - and mode of action studies of the N terminal, proline-rich region
(Journal article; Tidsskriftartikkel; Peer reviewed, 2012)Arasin 1 is a 37 amino acid long proline-rich antimicrobial peptide isolated from the spider crab, Hyas araneus. In this work the active region of arasin 1 was identified through structure-activity studies using different peptide fragments derived from the arasin 1 sequence. The pharmacophore was found to be located in the proline/arginine-rich NH2 terminus of the peptide and the fragment arasin ... -
Synthesis and Antimicrobial Activity of Short Analogues of the Marine Antimicrobial Peptide Turgencin A: Effects of SAR Optimizations, Cys-Cys Cyclization and Lipopeptide Modifications
(Journal article; Tidsskriftartikkel; Peer reviewed, 2022-11-10)We have synthesised short analogues of the marine antimicrobial peptide Turgencin A from the colonial Arctic ascidian Synoicum turgens. In this study, we focused on a central, cationic 12-residue Cys-Cys loop region within the sequence. Modified (tryptophan- and arginine-enriched) linear peptides were compared with Cys-Cys cyclic derivatives, and both linear and Cys-cyclic peptides were N-terminally ...
