Esposito, G.; Mai, L.H.; Longeon, A.; Mangoni, A.; Durieu, E.; Meijer, L.; Van Soest, R.; Costantino, V.; Bourguet-Kondracki, M.-L. (2019). A Collection of Bioactive Nitrogen-Containing Molecules from the Marine Sponge Acanthostrongylophora ingens. Marine Drugs. 17(8): 472.

430647

10.3390/md17080472 [view]

Esposito, G.; Mai, L.H.; Longeon, A.; Mangoni, A.; Durieu, E.; Meijer, L.; Van Soest, R.; Costantino, V.; Bourguet-Kondracki, M.-L.

2019

17(8): 472

Publication

Available for editors   [request]

Thirteen nitrogen-containing molecules (1a/1b and 2–12) were isolated from the Indonesian sponge Acanthostrongylophora ingens, 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 ?-42 assays. The most interesting bioactivity result was obtained with the known acanthocyclamine A (3), which revealed for the first time a specific Escherichia coli antimicrobial activity and an inhibitory e?ect on amyloid ?-42 production induced by aftin-5 and no cytotoxicity at the dose of 26 ?M. These results highlight the potentiality of a bipiperidine sca?old as a promising skeleton for preventing or reducing the production of amyloid ?-42, a key player in the initiation of Alzheimer’s disease.

Northern Indian Ocean

Chemistry

Porifera

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