Abstract：
: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 β-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 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.
journal_name
Mar Drugsjournal_title
Marine drugsauthors
Esposito G,Mai LH,Longeon A,Mangoni A,Durieu E,Meijer L,Van Soest R,Costantino V,Bourguet-Kondracki MLdoi
10.3390/md17080472subject
Has Abstractpub_date
2019-08-15 00:00:00issue
8issn
1660-3397pii
md17080472journal_volume
17pub_type
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