| Autor: |
Mora FD; Department of Pharmacognosy, and National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA., Jones DK, Desai PV, Patny A, Avery MA, Feller DR, Smillie T, Zhou YD, Nagle DG |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of natural products [J Nat Prod] 2006 Apr; Vol. 69 (4), pp. 547-52. |
| DOI: |
10.1021/np050397q |
| Abstrakt: |
Peroxisome proliferator-activated receptors (PPARs), members of the nuclear hormone receptor (NHR) family, are ligand-activated transcription factors. Ligands (agonists) of PPARgamma have been shown to inhibit growth, promote terminal differentiation, and induce apoptosis in human breast tumor cells. A cell-based reporter assay was developed to examine extracts of terrestrial and marine organisms for the ability to activate PPARgamma. Bioassay-guided fractionation and isolation of an active extract from Pseudoceratina rhax yielded the known histone deacetylase (HDAC) inhibitor psammaplin A (1). Compound 1 activates PPARgamma in a MCF-7 cell-based reporter assay and induces apoptosis in human breast tumor cells in vitro. Molecular modeling studies suggest that 1 may interact with binding sites within the PPARgamma ligand-binding pocket. Therefore, in addition to its known effects on HDAC-mediated processes, activation of PPARgamma-regulated gene expression may play a role in the ability of 1 to induce apoptosis. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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