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KMID : 0606320050220010001
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Journal of Phamacetical Sciences Sookmyung Women s University
2005 Volume.22 No. 1 p.1 ~ p.10
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Anti-inflammatory and Anti-angiogenic Actions of PCX-Series Compounds as Celecoxib Derivatives
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Soh Jee-Hyun
Ahn Eun-Kyung
Juhn Hye-Jin
Lim Eun-Joo
Park Eun-Hee
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Abstract
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This study aimed to evaluate the pharmacological efficacies of PCX-series compounds, which were synthesized as prodrugs of celecoxib, a COX-2 selective inhibitor. Celecoxib, PCX-1, PCX-2, PCX-3, PCX-7, PCX-15 and PCX-16 provide potent anti-angiogenic activity in chorioallantoic membrane (CAM) assay. In addition, celecoxib, PCX-2, and PCX-16 showed anti-angiogenic activity in a dose-dependent manner. PCX-2 inhibited swelling in the carrageenan-induced rat paw edema test 24 hours after the administration. In the acetic acid-induced writhing test, PCX-7 and PCX-15 were verified to provide more potent analgesic effect than celecoxib 12 hours after the administration, and PCX-2 showed potent analgesic effect 24 hours after the administration. In the carrageenan-induced rat air pouch model, PCX-2 significantly decreased exudate volume, number of leukocyte and NO level. In the ulcerogenic activity test, PCX-2, PCX-7, PCX-15, and PCX-16 showed significantly less ulcer formation than indomethacin. Especially, PCX-7 showed the highest safety in the GI safety test. These findings provide novel pharmacological knowledge on pharmacological actions of celecoxib and its PCX-series compouds.
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