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KMID : 0369820130430020101
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Jorunal of Korean Pharmaceutical Sciences
2013 Volume.43 No. 2 p.101 ~ p.106
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Antitumor effect of a newly synthesized celecoxib derivative encapsulated in liposome
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Kim Bee
Shin Dae-Hwan
Kim Hee-Doo
Kim Jin-Seok
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Abstract
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A new cyclooxygenase-2 inhibitor (code: PCX-3) was synthesized as a sodium salt form of celecoxib, a non-steroidal anti-inflammatory drug (NSAID), and tested for its anticancer activity using human colon adenocarcinoma cells (HT-29) in vitro. Anti-proliferative effect of HT-29 cells by PCX-3 in DPPC/Chol liposomes was more effective than the free PCX-3 by 2-folds (IC30 = 125 μM vs. 227.5 μM). The same liposomal formulation of PCX-3 also showed a 2-fold increased effect than the free one both in DNA fragmentation and caspase activity of HT-29 cells at 19-743 μM and 37?371 μM ranges, respectively, suggesting apoptosis-based anti-proliferative effect. Down regulation of prostaglandin E2 level of HT-29 cells by the treatment of liposomal PCX-3 was more profound than its free form at 0.001?0.002 μM range. These data suggest that the liposomal formulation of this newly synthesized PCX-3 could be re-visited as a new anticancer or chemo-preventive agent in the future.
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KEYWORD
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Celecoxib, Liposomes, Caspase, Anticancer drugs, COX-2
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