Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells.

Abstract

Klugine (1), isocephaeline (2), and emetine (4) inhibited hypoxia-inducible factor-1 (HIF-1) activation by hypoxia in T47D breast tumor cells (IC(50) values 0.2, 1.1, and 0.11 muM, respectively). Compounds 1, 2, and 4 inhibited both hypoxia- and iron chelator-induced HIF-1 activation by blocking HIF-1alpha protein accumulation.

• Authors: Yu-Dong Zhou, Yong-Pil Kim, Kaleem Asjad Mohammed, Deborah K Jones, Ilias Muhammad, D Chuck Dunbar, Dale G Nagle
• Journal: Journal of natural products (J Nat Prod) Vol. 68 Issue 6 Pg. 947-50 (Jun 2005) ISSN: 0163-3864 [Print] United States
• PMID: 15974627 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Alkaloids
• DNA-Binding Proteins
• HIF1A protein, human
• Hypoxia-Inducible Factor 1
• Hypoxia-Inducible Factor 1, alpha Subunit
• Nuclear Proteins
• Quinazolines
• Terpenes
• Tetrahydroisoquinolines
• Transcription Factors
• Vascular Endothelial Growth Factor A
• isocephaeline
• klugine
• Emetine

Topics

• Alkaloids (chemistry, pharmacology)
• Breast Neoplasms
• DNA-Binding Proteins (drug effects)
• Emetine (chemistry, pharmacology)
• Humans
• Hypoxia-Inducible Factor 1
• Hypoxia-Inducible Factor 1, alpha Subunit
• Molecular Structure
• Nuclear Proteins (drug effects)
• Quinazolines (chemistry, pharmacology)
• Rubiaceae (chemistry)
• Terpenes (chemistry, pharmacology)
• Tetrahydroisoquinolines (chemistry, pharmacology)
• Transcription Factors (drug effects)
• Tumor Cells, Cultured
• Vascular Endothelial Growth Factor A (analysis)