| A natural propenoic acid derivative activates peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta). | |
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MedLine Citation:
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PMID: 20153754 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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AIMS: Previous studies showed that natural prenyloxyphenylpropanoid derivatives have potent biological properties in vivo. Given the structural similarities between these compounds and known peroxisome proliferator-activated receptor (PPAR) agonists, the present study examined the hypothesis that propenoic acid derivatives activate PPARs. MAIN METHODS: Chimeric reporter assays were performed to identify propenoic acid derivates that could activate PPARs. Quantitative polymerase chain reaction (qPCR) analysis of wild-type and Pparbeta/delta-null mouse primary keratinocytes was performed to determine if a test compound could specifically activate PPARbeta/delta. A human epithelial carcinoma cell line and primary mouse keratinocytes were used to determine the effect of the compound on cell proliferation. KEY FINDINGS: Three of the propenoic acid derivatives activated PPARs, with the greatest efficacy being observed with prenyloxycinnamic acid derivatives 4'-geranyloxyferulic acid (compound 1) for PPARbeta/delta. Compound 1 increased expression of a known PPARbeta/delta target gene through a mechanism that requires PPARbeta/delta. Inhibition of cell proliferation by compound 1 was found in a human epithelial carcinoma cell line. SIGNIFICANCE: Results from these studies demonstrate that compound 1 can activate PPARbeta/delta and inhibit cell proliferation of a human skin cancer cell line, suggesting that the biological effects of 4'-geranyloxyferulic acid may be mediated in part by activating this PPAR isoform. |
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Authors:
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Salvatore Genovese; Jennifer E Foreman; Michael G Borland; Francesco Epifano; Frank J Gonzalez; Massimo Curini; Jeffrey M Peters |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural Date: 2010-02-12 |
Journal Detail:
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Title: Life sciences Volume: 86 ISSN: 1879-0631 ISO Abbreviation: Life Sci. Publication Date: 2010 Mar |
Date Detail:
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Created Date: 2010-03-22 Completed Date: 2010-04-12 Revised Date: 2011-07-27 |
Medline Journal Info:
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Nlm Unique ID: 0375521 Medline TA: Life Sci Country: Netherlands |
Other Details:
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Languages: eng Pagination: 493-8 Citation Subset: IM |
Copyright Information:
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Copyright 2010 Elsevier Inc. All rights reserved. |
Affiliation:
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Dipartimento di Scienze del Farmaco, Università G. D'Annunzio, Chieti-Pescara, Via dei Vestini 31, 66100 Chieti Scalo, Italy. |
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals COS Cells Cell Line Cell Line, Tumor Cell Proliferation / drug effects Cercopithecus aethiops Coumarins / chemistry, pharmacology Gene Expression Regulation / drug effects* Humans Mice Molecular Structure PPAR delta / metabolism* PPAR-beta / metabolism* Phenylpropionates / chemistry, pharmacology* Polymerase Chain Reaction Up-Regulation |
| Grant Support | |
ID/Acronym/Agency:
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CA124533/CA/NCI NIH HHS; CA126826/CA/NCI NIH HHS; CA141029/CA/NCI NIH HHS; R01 CA124533-03/CA/NCI NIH HHS; R01 CA124533-05/CA/NCI NIH HHS; R01 CA126826-01A2/CA/NCI NIH HHS; R01 CA141029-01A1/CA/NCI NIH HHS; R01 CA141029-02/CA/NCI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Coumarins; 0/PPAR delta; 0/PPAR-beta; 0/Phenylpropionates; 495-02-3/aurapten |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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