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Antitumor effect of a newly synthesized celecoxib derivative encapsulated in liposome

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Abstract

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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Authors and Affiliations

  1. College of Pharmacy, Sookmyung Women’s University, Chungpa-Dong 2-Ga, Youngsan-Gu, Seoul, South Korea

    Bee Kim, Dae Hwan Shin, Hee Doo Kim & Jin-Seok Kim

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  1. Bee Kim
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  2. Dae Hwan Shin
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  3. Hee Doo Kim
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  4. Jin-Seok Kim
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Correspondence to Jin-Seok Kim.

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The first two authors, Bee Kim and Dae Hwan Shin, equally contributed to this paper as co-first authors.

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Kim, B., Shin, D.H., Kim, H.D. et al. Antitumor effect of a newly synthesized celecoxib derivative encapsulated in liposome. Journal of Pharmaceutical Investigation 43, 101–106 (2013). https://doi.org/10.1007/s40005-013-0057-4

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  • DOI: https://doi.org/10.1007/s40005-013-0057-4

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