Differential anti-inflammatory and analgesic effects by enantiomers of zaltoprofen in rodents

• Published in: International immunopharmacology 2013-08, Vol.16 (4), p.457-460
• Main Authors: 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
• Format: Article
• Language: English
• 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
• ISSN: 1567-5769; 1878-1705
• DOI: 10.1016/j.intimp.2013.05.008

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.