English
norskBlar i forfatter "Strøm, Morten B."
Viser treff 1-13 av 13
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Amphipathic barbiturates as marine product mimics with cytolytic and immunogenic effects on head and neck squamous cell carcinoma cell lines
(Journal article; Tidsskriftartikkel; Peer reviewed, 2023-03-30)The incidence of head and neck squamous cell carcinoma (HNSCC) is increasing and the conventional treatments for this form of cancer can be tough. Despite the success of existing immunotherapies in some HNSCC patients, many do not respond to this type of treatment. Thus, the development of novel anti-cancer therapies should be prioritized. In the current study, the anticancer activity of a panel ... -
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 ... -
Amphipathic β2,2-Amino Acid Derivatives Suppress Infectivity and Disrupt the Intracellular Replication Cycle of Chlamydia Pneumoniae
(Journal article; Tidsskriftartikkel; Peer reviewed, 2016-06-09)We demonstrate in the current work that small cationic antimicrobial β2,2-amino acid derivatives (Mw < 500 Da) are highly potent against Chlamydia pneumoniae at clinical relevant concentrations (< 5 μM, i.e. < 3.4 μg/mL). C. pneumoniae is an atypical respiratory pathogen associated with frequent treatment failures and persistent infections. This gram-negative bacterium has a biphasic life cycle ... -
Antimicrobial activity of amphipathic α,α-disubstituted β-amino amide derivatives against ESBL–CARBA producing multi-resistant bacteria; effect of halogenation, lipophilicity and cationic character
(Journal article; Tidsskriftartikkel; Peer reviewed, 2019-09-06)The rapid emergence and spread of multi-resistant bacteria have created an urgent need for new antimicrobial agents. We report here a series of amphipathic α,α-disubstituted β-amino amide derivatives with activity against 30 multi-resistant clinical isolates of Gram-positive and Gram-negative bacteria, including isolates with extended spectrum β-lactamase – carbapenemase (ESBL-CARBA) production. A ... -
Antimicrobial activity of small synthetic peptides based on the marine peptide turgencin A: Prediction of antimicrobial peptide sequences in a natural peptide and strategy for optimization of potency
(Journal article; Tidsskriftartikkel; Peer reviewed, 2020-07-30)Turgencin A, a potent antimicrobial peptide isolated from the Arctic sea squirt <i>Synoicum turgens</i>, consists of 36 amino acid residues and three disulfide bridges, making it challenging to synthesize. The aim of the present study was to develop a truncated peptide with an antimicrobial drug lead potential based on turgencin A. The experiments consisted of: (1) sequence analysis and prediction ... -
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 ... -
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 ... -
The Marine Natural Product Mimic MHP88 Shows Anticancer Activity and has the Potential to Cause Immunogenic Cell Death
(Conference object; Konferansebidrag, 2020-03)The marine natural product mimic MHP 88 is a novel synthetic molecule based on unique structures found in molecules from an arctic marine bryozoan. Initial studies showed that MHP88 kills cancer cells efficiently, but is not hemolytic. In this study, we look closer at the mode of death induced by MHP88 in oral cancer (HSC-3) and lymphoma (Ramos) cell lines. Immunogenic cell death (ICD) is a mode of ... -
Methyl propiolate and 3-butynone: starting points for synthesis of amphiphilic 1,2,3-triazole peptidomimetics for antimicrobial evaluation
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-07-29)A library of 29 small 1,4-substituted 1,2,3-triazoles was prepared for studies of antimicrobial activity. The pharmacophore model investigated with these substrates was based on small peptidomimetics of antimicrobial peptides and antimicrobials isolated from marine organisms from sub-arctic regions. Using methyl 1,2,3-triazole-carboxylates and 1,2,3-triazole methyl ketones prepared through “click” ... -
Polymyxin B stabilized DNA micelles for sustained antibacterial and antibiofilm activity against P. aeruginosa
(Journal article; Tidsskriftartikkel; Peer reviewed, 2023-07-21)Nucleic acid-based materials showcase an increasing potential for antimicrobial drug delivery. Although numerous reports on drug-loaded DNA nanoparticles outline their pivotal antibacterial activities, their potential as drug delivery systems against bacterial biofilms awaits further studies. Among different oligonucleotide structures, micellar nanocarriers derived from amphiphilic DNA strands ... -
Screening for antibacterial and antifungal activities in marine benthic invertebrates from northern Norway
(Journal article; Tidsskriftartikkel; Peer reviewed, 2008-06-18)Benthic marine invertebrates collected from sub-Arctic regions of northern Norway, were found to be a promising source of novel bioactive compounds against human and fish pathogenic bacteria and fungi. Lyophilized material from seven species of ascidians, six sponges and one soft alcyonid coral were extracted with 60% acidified acetonitrile (ACN). After separation into an ACN-rich phase (ACN extract) ... -
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 ... -
Tailored anti-biofilm activity – Liposomal delivery for mimic of small antimicrobial peptide
(Journal article; Tidsskriftartikkel; Peer reviewed, 2023-12-13)The eradication of bacteria embedded in biofilms is among the most challenging obstacles in the management of chronic wounds. These biofilms are found in most chronic wounds; moreover, the biofilm-embedded bacteria are considerably less susceptible to conventional antimicrobial treatment than the planktonic bacteria. Antimicrobial peptides and their mimics are considered attractive candidates in the ...
