Food Polyphenols Fail to Cause a Biologically Relevant Reduction of COX-2 Activity
Epidemiologic studies show a correlation between the dietary intake of food polyphenols and beneficial health effects. Several in vitro studies indicate that the anti-inflammatory potential of polyphenols is, at least in part, mediated by a modulation of the enzymes of the arachidonic acid cascade,...
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| description | Epidemiologic studies show a correlation between the dietary intake of food polyphenols and beneficial health effects. Several in vitro studies indicate that the anti-inflammatory potential of polyphenols is, at least in part, mediated by a modulation of the enzymes of the arachidonic acid cascade, such as the prostaglandin forming cyclooxygenases (COXs). Evidence that this mode of action can be transferred to the situation in vivo is scarce. This study characterized effects of a subset of polyphenols on COX-2 expression and activity in vitro and compared the potency with known drugs. Next, the in vivo relevance of the observed in vitro effects was tested. Enzyme assays and incubations of polyphenols with the cancer cell line HCA-7 and lipopolysaccharide (LPS) stimulated primary monocytes support the hypothesis that polyphenols can effect COX-2 expression and activity in vitro. The effects were most pronounced in the monocyte assay for wogonin, apigenin, resveratrol and genistein with IC50 values of 1.5 μM, 2.6 μM, 2.8 μM and 7.4 μM. However, these values are 100- to 1000-fold higher in comparison to those of the known pharmaceuticals celecoxib, indomethacin and dexamethasone. In an animal model of LPS induced sepsis, pretreatment with polyphenols (i. p. 100 mg/kg bw) did not result in decreased plasma or tissue prostaglandin levels, whereas the positive control celecoxib effectively attenuated LPS induced prostaglandin formation. These data suggest that despite the moderate potency in vitro, an effect of polyphenols on COX-2 during acute inflammation is unlikely, even if a high dose of polyphenols is ingested. |
| doi_str_mv | 10.1371/journal.pone.0139147 |
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Several in vitro studies indicate that the anti-inflammatory potential of polyphenols is, at least in part, mediated by a modulation of the enzymes of the arachidonic acid cascade, such as the prostaglandin forming cyclooxygenases (COXs). Evidence that this mode of action can be transferred to the situation in vivo is scarce. This study characterized effects of a subset of polyphenols on COX-2 expression and activity in vitro and compared the potency with known drugs. Next, the in vivo relevance of the observed in vitro effects was tested. Enzyme assays and incubations of polyphenols with the cancer cell line HCA-7 and lipopolysaccharide (LPS) stimulated primary monocytes support the hypothesis that polyphenols can effect COX-2 expression and activity in vitro. The effects were most pronounced in the monocyte assay for wogonin, apigenin, resveratrol and genistein with IC50 values of 1.5 μM, 2.6 μM, 2.8 μM and 7.4 μM. However, these values are 100- to 1000-fold higher in comparison to those of the known pharmaceuticals celecoxib, indomethacin and dexamethasone. In an animal model of LPS induced sepsis, pretreatment with polyphenols (i. p. 100 mg/kg bw) did not result in decreased plasma or tissue prostaglandin levels, whereas the positive control celecoxib effectively attenuated LPS induced prostaglandin formation. These data suggest that despite the moderate potency in vitro, an effect of polyphenols on COX-2 during acute inflammation is unlikely, even if a high dose of polyphenols is ingested.</description><identifier>ISSN: 1932-6203</identifier><identifier>EISSN: 1932-6203</identifier><identifier>DOI: 10.1371/journal.pone.0139147</identifier><identifier>PMID: 26440517</identifier><language>eng</language><publisher>United States: Public Library of Science</publisher><subject>Analytical chemistry ; Animals ; Anti-Inflammatory Agents - pharmacology ; Apigenin - pharmacology ; Arachidonic acid ; Bioavailability ; Cancer ; Celecoxib ; Celecoxib - pharmacology ; Cell Line, Tumor ; Cells, Cultured ; Correlation analysis ; Cyclooxygenase 2 - metabolism ; Cyclooxygenase-2 ; Cyclooxygenases ; Cytotoxicity ; Dexamethasone ; Diet ; Dietary intake ; Enzyme Activation - drug effects ; Epidemiology ; Food ; Food intake ; Gene expression ; Genetic aspects ; Genistein ; Genistein - pharmacology ; Humans ; In vivo methods and tests ; Indomethacin ; Indomethacin - pharmacology ; Inflammation ; Inflammatory bowel disease ; Lipopolysaccharides ; Lipopolysaccharides - pharmacology ; Male ; Medical research ; Metabolites ; Mice, Inbred C57BL ; Mode of action ; Monocytes ; Monocytes - drug effects ; Monocytes - metabolism ; Nephrology ; Physiological aspects ; Polyphenols ; Polyphenols - pharmacology ; Real-Time Polymerase Chain Reaction ; Resveratrol ; Sepsis ; Stilbenes - pharmacology ; Studies ; Toxicology ; Veterinary medicine</subject><ispartof>PloS one, 2015-10, Vol.10 (10), p.e0139147</ispartof><rights>COPYRIGHT 2015 Public Library of Science</rights><rights>2015 Willenberg et al. This is an open access article distributed under the terms of the Creative Commons Attribution License: http://creativecommons.org/licenses/by/4.0/ (the “License”), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2015 Willenberg et al 2015 Willenberg et al</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c692t-68cd1def5efda5dc691c8bb769df2a1e327a711b785d04fade4f9dbe1b24c7483</citedby><cites>FETCH-LOGICAL-c692t-68cd1def5efda5dc691c8bb769df2a1e327a711b785d04fade4f9dbe1b24c7483</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4594923/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4594923/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,727,780,784,864,885,2101,2927,23865,27923,27924,53790,53792,79471,79472</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26440517$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><contributor>Scavone, Cristoforo</contributor><creatorcontrib>Willenberg, Ina</creatorcontrib><creatorcontrib>Meschede, Anna K</creatorcontrib><creatorcontrib>Gueler, Faikah</creatorcontrib><creatorcontrib>Jang, Mi-Sun</creatorcontrib><creatorcontrib>Shushakova, Nelli</creatorcontrib><creatorcontrib>Schebb, Nils Helge</creatorcontrib><title>Food Polyphenols Fail to Cause a Biologically Relevant Reduction of COX-2 Activity</title><title>PloS one</title><addtitle>PLoS One</addtitle><description>Epidemiologic studies show a correlation between the dietary intake of food polyphenols and beneficial health effects. Several in vitro studies indicate that the anti-inflammatory potential of polyphenols is, at least in part, mediated by a modulation of the enzymes of the arachidonic acid cascade, such as the prostaglandin forming cyclooxygenases (COXs). Evidence that this mode of action can be transferred to the situation in vivo is scarce. This study characterized effects of a subset of polyphenols on COX-2 expression and activity in vitro and compared the potency with known drugs. Next, the in vivo relevance of the observed in vitro effects was tested. Enzyme assays and incubations of polyphenols with the cancer cell line HCA-7 and lipopolysaccharide (LPS) stimulated primary monocytes support the hypothesis that polyphenols can effect COX-2 expression and activity in vitro. The effects were most pronounced in the monocyte assay for wogonin, apigenin, resveratrol and genistein with IC50 values of 1.5 μM, 2.6 μM, 2.8 μM and 7.4 μM. However, these values are 100- to 1000-fold higher in comparison to those of the known pharmaceuticals celecoxib, indomethacin and dexamethasone. In an animal model of LPS induced sepsis, pretreatment with polyphenols (i. p. 100 mg/kg bw) did not result in decreased plasma or tissue prostaglandin levels, whereas the positive control celecoxib effectively attenuated LPS induced prostaglandin formation. 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pharmacology</subject><subject>Humans</subject><subject>In vivo methods and tests</subject><subject>Indomethacin</subject><subject>Indomethacin - pharmacology</subject><subject>Inflammation</subject><subject>Inflammatory bowel disease</subject><subject>Lipopolysaccharides</subject><subject>Lipopolysaccharides - pharmacology</subject><subject>Male</subject><subject>Medical research</subject><subject>Metabolites</subject><subject>Mice, Inbred C57BL</subject><subject>Mode of action</subject><subject>Monocytes</subject><subject>Monocytes - drug effects</subject><subject>Monocytes - metabolism</subject><subject>Nephrology</subject><subject>Physiological aspects</subject><subject>Polyphenols</subject><subject>Polyphenols - pharmacology</subject><subject>Real-Time Polymerase Chain Reaction</subject><subject>Resveratrol</subject><subject>Sepsis</subject><subject>Stilbenes - pharmacology</subject><subject>Studies</subject><subject>Toxicology</subject><subject>Veterinary medicine</subject><issn>1932-6203</issn><issn>1932-6203</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><sourceid>DOA</sourceid><recordid>eNqNkm-r0zAUxoso3uvVbyBaEARfdCZp2rRvhDmcDi5M5h98F9LkZMvImtmkw317M9d7WUFB8iInJ7_zJDl5kuQ5RhOcM_x26_quFXaydy1MEM5rTNmD5BrXOclKgvKHF_FV8sT7LUJFXpXl4-SKlJSiArPrZDV3TqWfnT3uN9A669O5MDYNLp2J3kMq0vfGWbc2Ulh7TFdg4SDaEAPVy2BcmzqdzpY_MpJO4_pgwvFp8kgL6-HZMN8k3-Yfvs4-ZbfLj4vZ9DaTZU1CVlZSYQW6AK1EoWISy6ppWFkrTQSGnDDBMG5YVShEtVBAda0awA2hktEqv0lennX31nk-tMNzzOKzWUkRicTiTCgntnzfmZ3ojtwJw_8kXLfmogtGWuBABWWVJLSpYqDqRgCDppBNQ7QQCKLWu-G0vtmBktCGTtiR6HinNRu-dgdOi5rWJI8CrwaBzv3swYd_XHmg1iLeyrTaRTG5M17yKc1RRWtcnp4--QsVh4KdkdEQ2sT8qODNqCAyAX6FdfxjzxdfVv_PLr-P2dcX7AaEDRvvbH9yhh-D9AzKznnfgb7vHEb85Oe7bvCTn_ng51j24rLr90V3Bs5_Ay9y8R0</recordid><startdate>20151006</startdate><enddate>20151006</enddate><creator>Willenberg, Ina</creator><creator>Meschede, Anna K</creator><creator>Gueler, Faikah</creator><creator>Jang, Mi-Sun</creator><creator>Shushakova, Nelli</creator><creator>Schebb, Nils Helge</creator><general>Public Library of Science</general><general>Public Library of Science (PLoS)</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>IOV</scope><scope>ISR</scope><scope>3V.</scope><scope>7QG</scope><scope>7QL</scope><scope>7QO</scope><scope>7RV</scope><scope>7SN</scope><scope>7SS</scope><scope>7T5</scope><scope>7TG</scope><scope>7TM</scope><scope>7U9</scope><scope>7X2</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8C1</scope><scope>8FD</scope><scope>8FE</scope><scope>8FG</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABJCF</scope><scope>ABUWG</scope><scope>AEUYN</scope><scope>AFKRA</scope><scope>ARAPS</scope><scope>ATCPS</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>BHPHI</scope><scope>C1K</scope><scope>CCPQU</scope><scope>D1I</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>H94</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>KB.</scope><scope>KB0</scope><scope>KL.</scope><scope>L6V</scope><scope>LK8</scope><scope>M0K</scope><scope>M0S</scope><scope>M1P</scope><scope>M7N</scope><scope>M7P</scope><scope>M7S</scope><scope>NAPCQ</scope><scope>P5Z</scope><scope>P62</scope><scope>P64</scope><scope>PATMY</scope><scope>PDBOC</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>PTHSS</scope><scope>PYCSY</scope><scope>RC3</scope><scope>5PM</scope><scope>DOA</scope></search><sort><creationdate>20151006</creationdate><title>Food Polyphenols Fail to Cause a Biologically Relevant Reduction of COX-2 Activity</title><author>Willenberg, Ina ; Meschede, Anna K ; Gueler, Faikah ; Jang, Mi-Sun ; Shushakova, Nelli ; Schebb, Nils Helge</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c692t-68cd1def5efda5dc691c8bb769df2a1e327a711b785d04fade4f9dbe1b24c7483</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Analytical chemistry</topic><topic>Animals</topic><topic>Anti-Inflammatory Agents - pharmacology</topic><topic>Apigenin - pharmacology</topic><topic>Arachidonic acid</topic><topic>Bioavailability</topic><topic>Cancer</topic><topic>Celecoxib</topic><topic>Celecoxib - pharmacology</topic><topic>Cell Line, Tumor</topic><topic>Cells, Cultured</topic><topic>Correlation analysis</topic><topic>Cyclooxygenase 2 - metabolism</topic><topic>Cyclooxygenase-2</topic><topic>Cyclooxygenases</topic><topic>Cytotoxicity</topic><topic>Dexamethasone</topic><topic>Diet</topic><topic>Dietary intake</topic><topic>Enzyme Activation - drug effects</topic><topic>Epidemiology</topic><topic>Food</topic><topic>Food intake</topic><topic>Gene expression</topic><topic>Genetic aspects</topic><topic>Genistein</topic><topic>Genistein - pharmacology</topic><topic>Humans</topic><topic>In vivo methods and tests</topic><topic>Indomethacin</topic><topic>Indomethacin - pharmacology</topic><topic>Inflammation</topic><topic>Inflammatory bowel disease</topic><topic>Lipopolysaccharides</topic><topic>Lipopolysaccharides - 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Several in vitro studies indicate that the anti-inflammatory potential of polyphenols is, at least in part, mediated by a modulation of the enzymes of the arachidonic acid cascade, such as the prostaglandin forming cyclooxygenases (COXs). Evidence that this mode of action can be transferred to the situation in vivo is scarce. This study characterized effects of a subset of polyphenols on COX-2 expression and activity in vitro and compared the potency with known drugs. Next, the in vivo relevance of the observed in vitro effects was tested. Enzyme assays and incubations of polyphenols with the cancer cell line HCA-7 and lipopolysaccharide (LPS) stimulated primary monocytes support the hypothesis that polyphenols can effect COX-2 expression and activity in vitro. The effects were most pronounced in the monocyte assay for wogonin, apigenin, resveratrol and genistein with IC50 values of 1.5 μM, 2.6 μM, 2.8 μM and 7.4 μM. However, these values are 100- to 1000-fold higher in comparison to those of the known pharmaceuticals celecoxib, indomethacin and dexamethasone. In an animal model of LPS induced sepsis, pretreatment with polyphenols (i. p. 100 mg/kg bw) did not result in decreased plasma or tissue prostaglandin levels, whereas the positive control celecoxib effectively attenuated LPS induced prostaglandin formation. These data suggest that despite the moderate potency in vitro, an effect of polyphenols on COX-2 during acute inflammation is unlikely, even if a high dose of polyphenols is ingested.</abstract><cop>United States</cop><pub>Public Library of Science</pub><pmid>26440517</pmid><doi>10.1371/journal.pone.0139147</doi><oa>free_for_read</oa></addata></record> |
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| ispartof | PloS one, 2015-10, Vol.10 (10), p.e0139147 |
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| source | MEDLINE; DOAJ Directory of Open Access Journals; Public Library of Science (PLoS); EZB-FREE-00999 freely available EZB journals; PubMed Central; Free Full-Text Journals in Chemistry |
| subjects | Analytical chemistry Animals Anti-Inflammatory Agents - pharmacology Apigenin - pharmacology Arachidonic acid Bioavailability Cancer Celecoxib Celecoxib - pharmacology Cell Line, Tumor Cells, Cultured Correlation analysis Cyclooxygenase 2 - metabolism Cyclooxygenase-2 Cyclooxygenases Cytotoxicity Dexamethasone Diet Dietary intake Enzyme Activation - drug effects Epidemiology Food Food intake Gene expression Genetic aspects Genistein Genistein - pharmacology Humans In vivo methods and tests Indomethacin Indomethacin - pharmacology Inflammation Inflammatory bowel disease Lipopolysaccharides Lipopolysaccharides - pharmacology Male Medical research Metabolites Mice, Inbred C57BL Mode of action Monocytes Monocytes - drug effects Monocytes - metabolism Nephrology Physiological aspects Polyphenols Polyphenols - pharmacology Real-Time Polymerase Chain Reaction Resveratrol Sepsis Stilbenes - pharmacology Studies Toxicology Veterinary medicine |
| title | Food Polyphenols Fail to Cause a Biologically Relevant Reduction of COX-2 Activity |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-09T02%3A12%3A14IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-gale_plos_&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Food%20Polyphenols%20Fail%20to%20Cause%20a%20Biologically%20Relevant%20Reduction%20of%20COX-2%20Activity&rft.jtitle=PloS%20one&rft.au=Willenberg,%20Ina&rft.date=2015-10-06&rft.volume=10&rft.issue=10&rft.spage=e0139147&rft.pages=e0139147-&rft.issn=1932-6203&rft.eissn=1932-6203&rft_id=info:doi/10.1371/journal.pone.0139147&rft_dat=%3Cgale_plos_%3EA430849168%3C/gale_plos_%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=1719376402&rft_id=info:pmid/26440517&rft_galeid=A430849168&rft_doaj_id=oai_doaj_org_article_e4a478c24b8a47d9bae7eb5cbb2faa0e&rfr_iscdi=true |