A Collection of Bioactive Nitrogen-Containing Molecules from the Marine Sponge Acanthostrongylophora ingens

Thirteen nitrogen-containing molecules ( / and - ) were isolated from the Indonesian sponge , highlighting the richness of this organism as a source of alkaloids. Their structures were elucidated using one- and two-dimensional NMR spectroscopy and HR-ESI-MS, while the stereochemistry of the diketopi...

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Veröffentlicht in:Marine drugs 2019-08, Vol.17 (8), p.472
Hauptverfasser: Esposito, Germana, Mai, Linh H, Longeon, Arlette, Mangoni, Alfonso, Durieu, Emilie, Meijer, Laurent, Van Soest, Rob, Costantino, Valeria, Bourguet-Kondracki, Marie-Lise
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Sprache:eng
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Zusammenfassung:Thirteen nitrogen-containing molecules ( / and - ) were isolated from the Indonesian sponge , highlighting the richness of this organism as a source of alkaloids. Their structures were elucidated using one- and two-dimensional NMR spectroscopy and HR-ESI-MS, while the stereochemistry of the diketopiperazines was established using Marfey's method. All compounds were screened in our standard bioactivity assays, including antibacterial, antikinases, and amyloid β-42 assays. The most interesting bioactivity result was obtained with the known acanthocyclamine A ( ), which revealed for the first time a specific antimicrobial activity and an inhibitory effect on amyloid β-42 production induced by aftin-5 and no cytotoxicity at the dose of 26 µM. These results highlight the potentiality of a bipiperidine scaffold as a promising skeleton for preventing or reducing the production of amyloid β-42, a key player in the initiation of Alzheimer's disease.
ISSN:1660-3397
1660-3397
DOI:10.3390/md17080472