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

被引：7

作者：

Esposito, Germana ^{[1
]}

Mai, Linh H. ^{[2
]}

Longeon, Arlette ^{[2
]}

Mangoni, Alfonso ^{[1
]}

Durieu, Emilie ^{[3
]}

Meijer, Laurent ^{[3
]}

Van Soest, Rob ^{[4
]}

Costantino, Valeria ^{[1
]}

Bourguet-Kondracki, Marie-Lise ^{[2
]}

机构：

[1] Univ Naples Federico II, Dept Pharm, Blue Chem Lab, I-80138 Naples, Italy

[2] Museum Natl Hist Nat, UMR CNRS 7245, Lab Mol Commun & Adaptat Microorganismes, 57 Rue Cuvier CP 54, F-75005 Paris, France

[3] Perharidy Peninsula, ManRos Therapeut, F-29680 Roscoff, France

[4] Naturalis Biodivers Ctr, POB 9517, NL-2300 RA Leiden, Netherlands

来源：

MARINE DRUGS | 2019年 / 17卷 / 08期

关键词：

Acanthostrongylophora ingens; marine sponge; halicyclamine derivative; diketopiperazine; alkaloid; bipiperidine scaffold; kinase inhibitor; antimicrobial activity; inhibitor of amyloid beta-42;

D O I：

10.3390/md17080472

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 beta-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 beta-42 production induced by aftin-5 and no cytotoxicity at the dose of 26 mu M. These results highlight the potentiality of a bipiperidine scaffold as a promising skeleton for preventing or reducing the production of amyloid beta-42, a key player in the initiation of Alzheimer's disease.

引用

页数：13

共 15 条

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