Abstract：
:The activator protein-1 (AP-1) family of transcription factors, including the most common member c-Jun-c-Fos, participates in regulation of expression of numerous genes involved in proliferation, apoptosis, and tumorigenesis in response to a wide array of stimuli including pro-inflammatory cytokines, growth factors, stress, and tumor promoters. A number of plant polyphenols including curcumin, a yellow compound in the spice turmeric, have been shown to inhibit the activation of AP-1. Curcumin is a polyphenolic dienone that is potentially reactive as a Michael acceptor and also is a strong anti-oxidant. Multiple activities reported for curcumin, including inhibition of the stress-induced activation of AP-1, have been suggested to involve the anti-oxidant properties of curcumin. In the present study, a library of analogs of curcumin was screened for activity against the TPA-induced activation of AP-1 using the Panomics AP-1 Reporter 293 stable cell line which is designed for screening potential inhibitors. Numerous analogs were identified that were more active than curcumin, including analogs that were not anti-oxidants and analogs that were not Michael acceptors. Clearly, anti-oxidant activity or reactivity as a Michael acceptor is not an essential feature of active compounds. In addition, a number of analogs were identified that enhanced the TPA-induced activation of AP-1. The results from screening were confirmed using BV-2 microglial cells where curcumin and analogs were shown to inhibit LPS-induced COX-2 expression; analogs identified as more potent than curcumin in the screening assay were also more potent than curcumin in preventing COX-2 expression.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Weber WM,Hunsaker LA,Gonzales AM,Heynekamp JJ,Orlando RA,Deck LM,Vander Jagt DLdoi
10.1016/j.bcp.2006.07.007subject
Has Abstractpub_date
2006-10-16 00:00:00pages
928-40issue
8eissn
0006-2952issn
1873-2968pii
S0006-2952(06)00423-0journal_volume
72pub_type
杂志文章abstract：:Homocysteine has been shown to increase glutathione levels in C3H/10T1/2 Cl 8 cells. The present paper confirms that this increase was specific for non-dividing cells. Several other thiols and disulfides, including cysteamine, mercaptoethanol and dithioerythritol, also increased glutathione, but the specificity for qu...
journal_title：Biochemical pharmacology
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pub_type： 杂志文章
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(94)90173-2
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pub_type： 杂志文章
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更新日期：2017-12-15 00:00:00
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更新日期：2019-07-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2016.03.016
更新日期：2016-05-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章,评审
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(82)90341-0
更新日期：1982-03-15 00:00:00
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pub_type： 杂志文章
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journal_title：Biochemical pharmacology
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pub_type： 杂志文章
doi：10.1016/j.bcp.2016.08.020
更新日期：2016-10-15 00:00:00
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pub_type： 杂志文章
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journal_title：Biochemical pharmacology
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更新日期：2004-12-01 00:00:00
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journal_title：Biochemical pharmacology
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