Palau'amine and related oroidin alkaloids dibromophakellin and dibromophakellstatin inhibit the human 20s proteasome

Theresa A. Lansdell, Nicole M. Hewlett, Amanda P. Skoumbourdis, Matthew D. Fodor, Ian B. Seiple, Shun Su, Phil S. Baran, Ken S. Feldman, Jetze J. Tepe

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31 Scopus citations

Abstract

We report herein that the oroidin-derived alkaloids palau'amine (1), dibromophakellin (2), and dibromophakellstatin (3) inhibit the proteolytic activity of the human 20S proteasome as well as the i20S immunoproteasome catalytic core. Palau'amine is found to prevent the degradation of ubiquitinylated proteins, including IκBα, in cell culture, which may be indicative of the potential mechanism by which these agents exhibit their exciting cytotoxic and immunosuppressive properties.

Original languageEnglish (US)
Pages (from-to)980-985
Number of pages6
JournalJournal of Natural Products
Volume75
Issue number5
DOIs
StatePublished - May 25 2012

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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    Lansdell, T. A., Hewlett, N. M., Skoumbourdis, A. P., Fodor, M. D., Seiple, I. B., Su, S., Baran, P. S., Feldman, K. S., & Tepe, J. J. (2012). Palau'amine and related oroidin alkaloids dibromophakellin and dibromophakellstatin inhibit the human 20s proteasome. Journal of Natural Products, 75(5), 980-985. https://doi.org/10.1021/np300231f