Agelasine Diterpenoids and Cbl-b Inhibitory Ageliferins from the Coralline Demosponge Astrosclera willeyana
| Autor: | Heidi R. Bokesch, Kirk R. Gustafson, Emily A. Smith, Antony Wamiru, Dongdong Wang, Barry R. O'Keefe, Brice A P Wilson, Unwoo Kang, Wei Jiang, Ekaterina I. Goncharova, Donna Voeller, Stanley Lipkowitz |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Astrosclera willeyana
QH301-705.5 Stereochemistry Pharmaceutical Science Agelasine 010402 general chemistry Inhibitory postsynaptic potential 01 natural sciences chemistry.chemical_compound Demosponge Cbl-b inhibition Drug Discovery Ic50 values Immunomodulatory protein Biology (General) N-methyladenine Pharmacology Toxicology and Pharmaceutics (miscellaneous) Ageliferin bromopyrrole agelasine diterpenoids biology 010405 organic chemistry Chemistry ageliferins Alkaloid biology.organism_classification 0104 chemical sciences |
| Zdroj: | Marine Drugs Volume 19 Issue 7 Marine Drugs, Vol 19, Iss 361, p 361 (2021) |
| ISSN: | 1660-3397 |
| DOI: | 10.3390/md19070361 |
| Popis: | An extract of the coralline demosponge Astrosclera willeyana inhibited the ubiquitin ligase activity of the immunomodulatory protein Cbl-b. The bioassay-guided separation of the extract provided ten active compounds, including three new N-methyladenine-containing diterpenoids, agelasines W–Y (1–3), a new bromopyrrole alkaloid, N(1)-methylisoageliferin (4), and six known ageliferin derivatives (5–10). The structures of the new compounds were elucidated from their spectroscopic and spectrometric data, including IR, HRESIMS, and NMR, and by comparison with spectroscopic data in the literature. While all of the isolated compounds showed Cbl-b inhibitory activities, ageliferins (4–10) were the most potent metabolites, with IC50 values that ranged from 18 to 35 μM. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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