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Agelasine Diterpenoids and Cbl-b Inhibitory Ageliferins from the Coralline Demosponge Astrosclera willeyana

  1. Author:
    Jiang, Wei [ORCID]
    Wang,Dongdong [ORCID]
    Wilson,Brice [ORCID]
    Kang, Unwoo
    Bokesch, Heidi R
    Smith,Emily [ORCID]
    Wamiru,Antony
    Goncharova,Katya
    Voeller, Donna
    Lipkowitz, Stanley
    O'Keefe,Barry [ORCID]
    Gustafson,Kirk [ORCID]

  2. Author Address

    Marine Science & Technology Institute, College of Environmental Science & Engineering, Yangzhou University, Yangzhou 225127, China., Molecular Targets Program, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD 21702-1201, USA., Basic Science Program, Frederick National Laboratory for Cancer Research, National Institutes of Health, Frederick, MD 21702-1201, USA., Advanced Biomedical Computational Science, Frederick National Laboratory for Cancer Research, Frederick, MD 21702-1201, USA., Women 39;s Malignancies Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892-1578, USA., Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, National Institutes of Health, Frederick, MD 21702-1201, USA.,
    1. Year: 2021
    2. Date: Jun 24
    3. Epub Date: 2021 06 24
  2. Journal: Marine drugs
    1. 19
    2. 7
  4. Type of Article: Article
  5. Article Number: 361
  6. ISSN: 1660-3397
  1. Abstract:

    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.

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External Sources

  1. View Full Text
  2. DOI: 10.3390/md19070361
  3. PMID: 34202500
  4. View record in Web of Science®
  5. WOS: 000677382800001
  6. PII : md19070361

Library Notes

  1. Fiscal Year: FY2020-2021
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