Original Article

The Effect of 3-Benzoyl-4-Phenyl-1-Methyl-4-Piperidinol Hydrochloride on Cox-1 and Cox-2 Enzyme Activities

  • H. Inci GÜL
  • Juan CATURLA
  • Merce AMAT

Received Date: 04.01.2005 Accepted Date: 04.07.2005 Turk J Pharm Sci 2005;2(2):105-109

Abstract Antiinflammatory activity of 3-benzoyl-4-phenyl-1-methyl-4-piperidinol hydrochloride (C1), which is semi-cyclic Mannich base, has been reported. In this study, the effects of the compound C1 on cyclooxygenase-1 (COX-1) and cyclooxygenase (COX-2) enzyme activities have been investigated as apossible mechanism of action for its anti-inflammatory activity. COX-2 activity was inhibited by 55% by C1 at 10 uM by 24 h. On the other hand, inhibition of COX-1 activity by C1 was negligible. Our results showed that C1 has selective inhibition on COX-2 activity, which prevents inflammation without having side effects such as gastric ulcer and hemorrhage. C1 can be a model compound to develop new anti-inflammatory compounds with COX-2 inhibiting activity. Özet Semi-siklik Mannich bazi olan 3-Benzoil-4-fenil-1-metil-4-piperidinol hidroklorür`ün (C1) antiinflamatuvar etkisi rapor edilmistir. Bu çalismada, C1 bilesiginin antiinflamatuvar aktivitesi için olasi etki mekanizmasi olarak siklooksijenaz-1 (COX-1) ve siklooksijenaz-2 (COX-2) enzim aktiviteleri üzerindeki etkileri arastirilmistir. C1 tarafindan COX-2 aktivitesinin inhibisyonu belirgindi: 24 satte 10 uM`da % 55. Diger taraftan, C1 tarafindan COX-1 aktivitesinin inhibisyonu ihmal edilebilir düzeydeydi. Sonuçlarimiz C1`in gastric ülser ve hemoraji gibi yan etkilere sahip olmaksizin inflamasyonu önleyen seçici COX-2 aktivitesi inhibisyonuna sahip oldugunu gösterdi. C1 COX-2 inhibe edici etkiye sahip yeni antienflamatuvar bilesiklerin gelistirilmesinde model bir bilesik olabilir.

Keywords: COX-1, COX-2, inflammation, Mannich base, piperidine.