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Bioactive Metabolites of Marine Origin Have Unusual Effects on Model Membrane Systems

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Department of Biological Sciences, University of Bergen, Thormøhlensgate 55, NO-5006 Bergen, Norway
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Department of Environmental Chemistry, Norwegian Geotechnical Institute, Sognsveien 72, 0855 Oslo, Norway
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Department of Chemistry, University of Oslo, P.O. Box 1033, Blindern, NO-0315 Oslo, Norway
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University of Antwerp, Laboratory of Microbiology, Parasitology and Hygiene, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Universiteitsplein 1, B-2610 Antwerp, Belgium
*
Authors to whom correspondence should be addressed.
Mar. Drugs 2020, 18(2), 125; https://doi.org/10.3390/md18020125
Received: 3 January 2020 / Revised: 4 February 2020 / Accepted: 12 February 2020 / Published: 19 February 2020
Marine sponges and soft corals have yielded novel compounds with antineoplastic and antimicrobial activities. Their mechanisms of action are poorly understood, and in most cases, little relevant experimental evidence is available on this topic. In the present study, we investigated whether agelasine D (compound 1) and three agelasine analogs (compound 24) as well as malonganenone J (compound 5), affect the physical properties of a simple lipid model system, consisting of dioleoylphospahtidylcholine and dioleoylphosphatidylethanolamine. The data indicated that all the tested compounds increased stored curvature elastic stress, and therefore, tend to deform the bilayer which occurs without a reduction in the packing stress of the hexagonal phase. Furthermore, lower concentrations (1%) appear to have a more pronounced effect than higher ones (5–10%). For compounds 4 and 5, this effect is also reflected in phospholipid headgroup mobility assessed using 31P chemical shift anisotropy (CSA) values of the lamellar phases. Among the compounds tested, compound 4 stands out with respect to its effects on the membrane model systems, which matches its efficacy against a broad spectrum of pathogens. Future work that aims to increase the pharmacological usefulness of these compounds could benefit from taking into account the compound effects on the fluid lamellar phase at low concentrations. View Full-Text
Keywords: agelasine; malonganenone; phase behavior; lipids; membrane affecting drug candidates; 31P NMR agelasine; malonganenone; phase behavior; lipids; membrane affecting drug candidates; 31P NMR
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MDPI and ACS Style

Jakubec, M.; Totland, C.; Rise, F.; Chamgordani, E.J.; Paulsen, B.; Maes, L.; Matheeussen, A.; Gundersen, L.-L.; Halskau, Ø. Bioactive Metabolites of Marine Origin Have Unusual Effects on Model Membrane Systems. Mar. Drugs 2020, 18, 125.

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