Hydrolytic Activity Is Essential for Aceclofenac To Inhibit Cyclooxygenase in Rheumatoid Synovial Cells
作者： Shusuke Hashimoto , Renzo Okamoto , Takeshi Matsuzaki , Yutaka Mizushima , Ryuta Yamazaki
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摘要: To investigate the mechanisms of action underlying anti-inflammatory effects nonsteroidal drug aceclofenac in humans, we studied metabolism detail primary cultured synovial cells 10 patients with rheumatoid arthritis. Aceclofenac and 4'-hydroxyaceclofenac are major compounds human blood after administration aceclofenac, but they had no inhibitory on cyclooxygenase (COX) activity or COX expression cells. In contrast, reduced prostaglandin E2 (PGE2) production by We also observed that were hydrolyzed into inhibitors diclofenac 4'-hydroxydiclofenac, respectively, However, hydrolytic differed markedly among cell preparations. Because suppressive potency against PGE2 was proportionally correlated preparations, suggest 4'-hydroxy facilitated
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