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Effects of compound 209 on colorectal cancer cell HT-29 in vivo and in vitro

Xiao Jiang, Xia Yuan, Mingming Chu, Wei Guo, Jingtao Liu, Fuxiang Ran, Zemei Ge, Runtao Li*, Jingrong Cui*   

  1. 1. State Key Laboratory of Natural and Biomimetic Drugs, Peking University Health Science Center, Beijing 100191, China
    2. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2012-09-30 Revised:2012-12-06 Online:2013-01-20 Published:2013-01-20
  • Contact: Runtao Li*, Jingrong Cui*

Abstract:

Compound 209 is a newly synthesized dithiocarbamate derivative with antiproliferation activity in vitro, however, its antitumor effect in vivo and the underlying mechanisms have yet to be identified. We explored the antitumor effect of compound 209 and the possible mechanisms for its inhibition of the growth of HT-29 xenograft tumor and proliferation of HT-29 cells. Cell proliferation was evaluated with SRB assay in vitro. The results showed that compound 209 had significant antiproliferation activity on HT-29 cells. Furthermore, the xenograft HT-29 nude mouse model was used to study the antitumor effect of compound 209 in vivo. We found that compound 209 significantly inhibited tumor growth and did not cause loss of body weight or leukocytopenia. Analysis by flow cytometry indicated that compound 209 arrested HT-29 cell cycle in G1 phase. Western blotting analysis suggested that compound 209 increased the expression of p27, cyclin E, CDK2, cyclin D1 and CDK4. These results demonstrated the antitumor effect of compound 209 and its potential use as an anticancer drug.

Key words: Dithiocarbamate, Compound 209, Cell cycle, Cell cycle-related proteins, HT-29 cell line

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