Differential anti-inflammatory and analgesic effects by enantiomers of zaltoprofen in rodents
In the present study, we investigated the effect of zaltoprofen enantiomers on inflammation and pain and compared their effect with racemic zaltoprofen. S(+)-zaltoprofen potently inhibited the inflammatory response in carrageenan-induced paw edema model, whereas R(−)-zaltoprofen did not. Moreover, t...
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creator | Cho, Ig Jun Lee, Chang Woo Lee, Myeong Youl Kang, Moo Rim Yun, Jieun Oh, Soo Jin Han, Sang-Bae Lee, Kiho Park, Song-Kyu Kim, Hwan Mook Jung, Sang-Hun Kang, Jong Soon |
description | In the present study, we investigated the effect of zaltoprofen enantiomers on inflammation and pain and compared their effect with racemic zaltoprofen. S(+)-zaltoprofen potently inhibited the inflammatory response in carrageenan-induced paw edema model, whereas R(−)-zaltoprofen did not. Moreover, the anti-inflammatory effect of S(+)-zaltoprofen was stronger than that of racemic zaltoprofen, suggesting that S(+)-zaltoprofen is an active component of racemic zaltoprofen in terms of anti-inflammatory activity. In contrast, the results of acetic acid-induced writhing model demonstrated that no significant analgesic effect was observed by racemic zaltoprofen and zaltoprofen enantiomers at doses used in carrageenan-induced paw edema model. However, racemic zaltoprofen and zaltoprofen enantiomers all exerted an analgesic effect at higher doses, which is inconsistent with the result of carrageenan-induced paw edema model. Gastric ulcers induced by racemic zaltoprofen and zaltoprofen enantiomers were minimal. Taken together, these results suggest that S(+)-zaltoprofen is a potent and active anti-inflammatory component of racemic zaltoprofen, but both S(+)-zaltoprofen and R(−)-zaltoprofen might seem to contribute to the analgesic effect of racemic zaltoprofen.
•S(+)-zaltoprofen is an active anti-inflammatory component of racemic zaltoprofen.•Both enantiomers of zaltoprofen contribute to the analgesic effect of racemate.•The effects of S(+)-zaltoprofen is more potent than the racemic zaltoprofen.•S(+)-zaltoprofen exerts minimal gastric damage. |
doi_str_mv | 10.1016/j.intimp.2013.05.008 |
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•S(+)-zaltoprofen is an active anti-inflammatory component of racemic zaltoprofen.•Both enantiomers of zaltoprofen contribute to the analgesic effect of racemate.•The effects of S(+)-zaltoprofen is more potent than the racemic zaltoprofen.•S(+)-zaltoprofen exerts minimal gastric damage.</description><identifier>ISSN: 1567-5769</identifier><identifier>EISSN: 1878-1705</identifier><identifier>DOI: 10.1016/j.intimp.2013.05.008</identifier><identifier>PMID: 23721690</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Analgesic ; Analgesics, Non-Narcotic - administration & dosage ; Analgesics, Non-Narcotic - adverse effects ; Analgesics, Non-Narcotic - chemistry ; Analgesics, Non-Narcotic - therapeutic use ; Animals ; Anti-inflammatory ; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage ; Anti-Inflammatory Agents, Non-Steroidal - adverse effects ; Anti-Inflammatory Agents, Non-Steroidal - chemistry ; Anti-Inflammatory Agents, Non-Steroidal - therapeutic use ; Benzopyrans - administration & dosage ; Benzopyrans - adverse effects ; Benzopyrans - chemistry ; Benzopyrans - therapeutic use ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Edema - drug therapy ; Enantiomer ; Male ; Mice ; Mice, Inbred ICR ; Pain - drug therapy ; Propionates - administration & dosage ; Propionates - adverse effects ; Propionates - chemistry ; Propionates - therapeutic use ; Rats ; Rats, Sprague-Dawley ; Stereoisomerism ; Stomach Ulcer - chemically induced ; Structure-Activity Relationship ; Zaltoprofen</subject><ispartof>International immunopharmacology, 2013-08, Vol.16 (4), p.457-460</ispartof><rights>2013 Elsevier B.V.</rights><rights>Copyright © 2013 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c461t-9c8a3864610dab17c24e501485d2c71198757d1343e1ccd74b93239c9cf4fe533</citedby><cites>FETCH-LOGICAL-c461t-9c8a3864610dab17c24e501485d2c71198757d1343e1ccd74b93239c9cf4fe533</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.intimp.2013.05.008$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23721690$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cho, Ig Jun</creatorcontrib><creatorcontrib>Lee, Chang Woo</creatorcontrib><creatorcontrib>Lee, Myeong Youl</creatorcontrib><creatorcontrib>Kang, Moo Rim</creatorcontrib><creatorcontrib>Yun, Jieun</creatorcontrib><creatorcontrib>Oh, Soo Jin</creatorcontrib><creatorcontrib>Han, Sang-Bae</creatorcontrib><creatorcontrib>Lee, Kiho</creatorcontrib><creatorcontrib>Park, Song-Kyu</creatorcontrib><creatorcontrib>Kim, Hwan Mook</creatorcontrib><creatorcontrib>Jung, Sang-Hun</creatorcontrib><creatorcontrib>Kang, Jong Soon</creatorcontrib><title>Differential anti-inflammatory and analgesic effects by enantiomers of zaltoprofen in rodents</title><title>International immunopharmacology</title><addtitle>Int Immunopharmacol</addtitle><description>In the present study, we investigated the effect of zaltoprofen enantiomers on inflammation and pain and compared their effect with racemic zaltoprofen. S(+)-zaltoprofen potently inhibited the inflammatory response in carrageenan-induced paw edema model, whereas R(−)-zaltoprofen did not. Moreover, the anti-inflammatory effect of S(+)-zaltoprofen was stronger than that of racemic zaltoprofen, suggesting that S(+)-zaltoprofen is an active component of racemic zaltoprofen in terms of anti-inflammatory activity. In contrast, the results of acetic acid-induced writhing model demonstrated that no significant analgesic effect was observed by racemic zaltoprofen and zaltoprofen enantiomers at doses used in carrageenan-induced paw edema model. However, racemic zaltoprofen and zaltoprofen enantiomers all exerted an analgesic effect at higher doses, which is inconsistent with the result of carrageenan-induced paw edema model. Gastric ulcers induced by racemic zaltoprofen and zaltoprofen enantiomers were minimal. Taken together, these results suggest that S(+)-zaltoprofen is a potent and active anti-inflammatory component of racemic zaltoprofen, but both S(+)-zaltoprofen and R(−)-zaltoprofen might seem to contribute to the analgesic effect of racemic zaltoprofen.
•S(+)-zaltoprofen is an active anti-inflammatory component of racemic zaltoprofen.•Both enantiomers of zaltoprofen contribute to the analgesic effect of racemate.•The effects of S(+)-zaltoprofen is more potent than the racemic zaltoprofen.•S(+)-zaltoprofen exerts minimal gastric damage.</description><subject>Analgesic</subject><subject>Analgesics, Non-Narcotic - administration & dosage</subject><subject>Analgesics, Non-Narcotic - adverse effects</subject><subject>Analgesics, Non-Narcotic - chemistry</subject><subject>Analgesics, Non-Narcotic - therapeutic use</subject><subject>Animals</subject><subject>Anti-inflammatory</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - adverse effects</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - chemistry</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - therapeutic use</subject><subject>Benzopyrans - administration & dosage</subject><subject>Benzopyrans - adverse effects</subject><subject>Benzopyrans - chemistry</subject><subject>Benzopyrans - therapeutic use</subject><subject>Disease Models, Animal</subject><subject>Dose-Response Relationship, Drug</subject><subject>Edema - drug therapy</subject><subject>Enantiomer</subject><subject>Male</subject><subject>Mice</subject><subject>Mice, Inbred ICR</subject><subject>Pain - drug therapy</subject><subject>Propionates - administration & dosage</subject><subject>Propionates - adverse effects</subject><subject>Propionates - chemistry</subject><subject>Propionates - therapeutic use</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Stereoisomerism</subject><subject>Stomach Ulcer - chemically induced</subject><subject>Structure-Activity Relationship</subject><subject>Zaltoprofen</subject><issn>1567-5769</issn><issn>1878-1705</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU-LFDEQxYMo7rr6DUT66KXbqk7S6b4Isv6FBS96lJBJKpKhuzMmPcL46a1hVo96CFUUv3oV3hPiOUKHgMOrfZfWLS2HrgeUHegOYHwgrnE0Y4sG9EPu9WBabYbpSjypdQ_Ac4WPxVUvTY_DBNfi29sUIxViKTc3jkub1ji7ZXFbLieeBH5u_k41-YaY9VttdqeG1jOcFyq1ybH55eYtH0qOtDZpbUoOLFmfikfRzZWe3dcb8fX9uy-3H9u7zx8-3b65a70acGsnPzo5DtxDcDs0vlekAdWoQ-8N4jQabQJKJQm9D0btJtnLyU8-qkhayhvx8qLLP_hxpLrZJVVP8-xWysdqUQMYA1Lp_6NyMBqYHRlVF9SXXGuhaA8lLa6cLII9Z2D39pKBPWdgQVvOgNde3F847hYKf5f-mM7A6wtAbMnPRMVWn2j1FFJhe23I6d8XfgPGhZoJ</recordid><startdate>20130801</startdate><enddate>20130801</enddate><creator>Cho, Ig Jun</creator><creator>Lee, Chang Woo</creator><creator>Lee, Myeong Youl</creator><creator>Kang, Moo Rim</creator><creator>Yun, Jieun</creator><creator>Oh, Soo Jin</creator><creator>Han, Sang-Bae</creator><creator>Lee, Kiho</creator><creator>Park, Song-Kyu</creator><creator>Kim, Hwan Mook</creator><creator>Jung, Sang-Hun</creator><creator>Kang, Jong Soon</creator><general>Elsevier B.V</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>7X8</scope><scope>7T5</scope><scope>H94</scope></search><sort><creationdate>20130801</creationdate><title>Differential anti-inflammatory and analgesic effects by enantiomers of zaltoprofen in rodents</title><author>Cho, Ig Jun ; Lee, Chang Woo ; Lee, Myeong Youl ; Kang, Moo Rim ; Yun, Jieun ; Oh, Soo Jin ; Han, Sang-Bae ; Lee, Kiho ; Park, Song-Kyu ; Kim, Hwan Mook ; Jung, Sang-Hun ; Kang, Jong Soon</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c461t-9c8a3864610dab17c24e501485d2c71198757d1343e1ccd74b93239c9cf4fe533</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>Analgesic</topic><topic>Analgesics, Non-Narcotic - administration & dosage</topic><topic>Analgesics, Non-Narcotic - adverse effects</topic><topic>Analgesics, Non-Narcotic - chemistry</topic><topic>Analgesics, Non-Narcotic - therapeutic use</topic><topic>Animals</topic><topic>Anti-inflammatory</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - adverse effects</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - chemistry</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - therapeutic use</topic><topic>Benzopyrans - administration & dosage</topic><topic>Benzopyrans - adverse effects</topic><topic>Benzopyrans - chemistry</topic><topic>Benzopyrans - therapeutic use</topic><topic>Disease Models, Animal</topic><topic>Dose-Response Relationship, Drug</topic><topic>Edema - drug therapy</topic><topic>Enantiomer</topic><topic>Male</topic><topic>Mice</topic><topic>Mice, Inbred ICR</topic><topic>Pain - drug therapy</topic><topic>Propionates - administration & dosage</topic><topic>Propionates - adverse effects</topic><topic>Propionates - chemistry</topic><topic>Propionates - therapeutic use</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Stereoisomerism</topic><topic>Stomach Ulcer - chemically induced</topic><topic>Structure-Activity Relationship</topic><topic>Zaltoprofen</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cho, Ig Jun</creatorcontrib><creatorcontrib>Lee, Chang Woo</creatorcontrib><creatorcontrib>Lee, Myeong Youl</creatorcontrib><creatorcontrib>Kang, Moo Rim</creatorcontrib><creatorcontrib>Yun, Jieun</creatorcontrib><creatorcontrib>Oh, Soo Jin</creatorcontrib><creatorcontrib>Han, Sang-Bae</creatorcontrib><creatorcontrib>Lee, Kiho</creatorcontrib><creatorcontrib>Park, Song-Kyu</creatorcontrib><creatorcontrib>Kim, Hwan Mook</creatorcontrib><creatorcontrib>Jung, Sang-Hun</creatorcontrib><creatorcontrib>Kang, Jong Soon</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Immunology Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><jtitle>International immunopharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cho, Ig Jun</au><au>Lee, Chang Woo</au><au>Lee, Myeong Youl</au><au>Kang, Moo Rim</au><au>Yun, Jieun</au><au>Oh, Soo Jin</au><au>Han, Sang-Bae</au><au>Lee, Kiho</au><au>Park, Song-Kyu</au><au>Kim, Hwan Mook</au><au>Jung, Sang-Hun</au><au>Kang, Jong Soon</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Differential anti-inflammatory and analgesic effects by enantiomers of zaltoprofen in rodents</atitle><jtitle>International immunopharmacology</jtitle><addtitle>Int Immunopharmacol</addtitle><date>2013-08-01</date><risdate>2013</risdate><volume>16</volume><issue>4</issue><spage>457</spage><epage>460</epage><pages>457-460</pages><issn>1567-5769</issn><eissn>1878-1705</eissn><abstract>In the present study, we investigated the effect of zaltoprofen enantiomers on inflammation and pain and compared their effect with racemic zaltoprofen. S(+)-zaltoprofen potently inhibited the inflammatory response in carrageenan-induced paw edema model, whereas R(−)-zaltoprofen did not. Moreover, the anti-inflammatory effect of S(+)-zaltoprofen was stronger than that of racemic zaltoprofen, suggesting that S(+)-zaltoprofen is an active component of racemic zaltoprofen in terms of anti-inflammatory activity. In contrast, the results of acetic acid-induced writhing model demonstrated that no significant analgesic effect was observed by racemic zaltoprofen and zaltoprofen enantiomers at doses used in carrageenan-induced paw edema model. However, racemic zaltoprofen and zaltoprofen enantiomers all exerted an analgesic effect at higher doses, which is inconsistent with the result of carrageenan-induced paw edema model. Gastric ulcers induced by racemic zaltoprofen and zaltoprofen enantiomers were minimal. Taken together, these results suggest that S(+)-zaltoprofen is a potent and active anti-inflammatory component of racemic zaltoprofen, but both S(+)-zaltoprofen and R(−)-zaltoprofen might seem to contribute to the analgesic effect of racemic zaltoprofen.
•S(+)-zaltoprofen is an active anti-inflammatory component of racemic zaltoprofen.•Both enantiomers of zaltoprofen contribute to the analgesic effect of racemate.•The effects of S(+)-zaltoprofen is more potent than the racemic zaltoprofen.•S(+)-zaltoprofen exerts minimal gastric damage.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>23721690</pmid><doi>10.1016/j.intimp.2013.05.008</doi><tpages>4</tpages></addata></record> |
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subjects | Analgesic Analgesics, Non-Narcotic - administration & dosage Analgesics, Non-Narcotic - adverse effects Analgesics, Non-Narcotic - chemistry Analgesics, Non-Narcotic - therapeutic use Animals Anti-inflammatory Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - adverse effects Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - therapeutic use Benzopyrans - administration & dosage Benzopyrans - adverse effects Benzopyrans - chemistry Benzopyrans - therapeutic use Disease Models, Animal Dose-Response Relationship, Drug Edema - drug therapy Enantiomer Male Mice Mice, Inbred ICR Pain - drug therapy Propionates - administration & dosage Propionates - adverse effects Propionates - chemistry Propionates - therapeutic use Rats Rats, Sprague-Dawley Stereoisomerism Stomach Ulcer - chemically induced Structure-Activity Relationship Zaltoprofen |
title | Differential anti-inflammatory and analgesic effects by enantiomers of zaltoprofen in rodents |
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