A Collection of Bioactive Nitrogen-Containing Molecules from the Marine Sponge Acanthostrongylophora ingens
| Autor: | Valeria Costantino, Alfonso Mangoni, Linh H. Mai, Laurent Meijer, Arlette Longeon, Emilie Durieu, Rob W. M. Van Soest, Germana Esposito, Marie-Lise Bourguet-Kondracki |
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| Přispěvatelé: | Centre d'Etude et de Recherche Travail Organisation Pouvoir (CERTOP), Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Université Toulouse - Jean Jaurès (UT2J), Laboratoire de chimie et biochimie des substances naturelles, Centre National de la Recherche Scientifique (CNRS)-Muséum national d'Histoire naturelle (MNHN), Università degli studi di Napoli Federico II, Molécules et cibles thérapeutiques (MCT), Station biologique de Roscoff [Roscoff] (SBR), Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), Université Toulouse - Jean Jaurès (UT2J), Université de Toulouse (UT)-Université de Toulouse (UT)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Centre National de la Recherche Scientifique (CNRS), Muséum national d'Histoire naturelle (MNHN)-Centre National de la Recherche Scientifique (CNRS), University of Naples Federico II = Università degli studi di Napoli Federico II, Esposito, Germana, Mai, Linh H., Longeon, Arlette, Mangoni, Alfonso, Durieu, Emilie, Meijer, Laurent, Van Soest, Rob, Costantino, Valeria, Bourguet-Kondracki, Marie-Lise |
| Jazyk: | angličtina |
| Rok vydání: | 2019 |
| Předmět: |
Amyloid
kinase inhibitor Pharmaceutical Science 010402 general chemistry medicine.disease_cause 01 natural sciences [CHIM.ANAL]Chemical Sciences/Analytical chemistry Drug Discovery medicine [CHIM]Chemical Sciences Cytotoxicity Pharmacology Toxicology and Pharmaceutics (miscellaneous) Diketopiperazines Escherichia coli lcsh:QH301-705.5 bipiperidine scaffold ComputingMilieux_MISCELLANEOUS antimicrobial activity biology 010405 organic chemistry Chemistry Alkaloid diketopiperazine inhibitor of amyloid β-42 Nuclear magnetic resonance spectroscopy halicyclamine derivative Antimicrobial biology.organism_classification alkaloid 3. Good health 0104 chemical sciences Acanthostrongylophora ingen Sponge Biochemistry lcsh:Biology (General) Acanthostrongylophora ingens marine sponge |
| Zdroj: | Marine drugs Marine drugs, MDPI, 2019, 17 (8), pp.472. ⟨10.3390/md17080472⟩ Marine Drugs, Vol 17, Iss 8, p 472 (2019) Marine drugs, 2019, 17 (8), pp.472. ⟨10.3390/md17080472⟩ Marine Drugs Volume 17 Issue 8 |
| ISSN: | 1660-3397 |
| DOI: | 10.3390/md17080472⟩ |
| Popis: | Thirteen nitrogen-containing molecules (1a/1b and 2&ndash 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&rsquo 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 µ 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&rsquo s disease. |
| Databáze: | OpenAIRE |
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