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高等学校化学研究 ›› 2010, Vol. 26 ›› Issue (3): 398-401.

• Articles • 上一篇    下一篇

Discovery of Fuchsone Derivatives as Novel Nonpeptide Inhibitor of Caspase-3

ZHANG Jin-liang1, LIU Sen1, GAO Chao-hui1, CHEN Xiao-song1, GUO Yang-hong2, WANG En-si3, FANG Xue-xun1 and WANG Ji-dong1*   

  1. 1. College of Life Science;
    2. College of Chemistry;
    3. School of Pharmaceutical Sciences, Jilin University, Changchun 130021, P. R. China
  • 收稿日期:2009-05-25 修回日期:2009-10-21 出版日期:2010-05-25 发布日期:2010-07-27
  • 通讯作者: WANG Ji-dong. E-mail: deepseasoncn@yahoo.com.cn
  • 基金资助:

    Supported by the National Natural Science Foundation of China(No.30371675) and the Foundation of Science & Technology Department of Jilin Province, China (No.20040543).

Discovery of Fuchsone Derivatives as Novel Nonpeptide Inhibitor of Caspase-3

ZHANG Jin-liang1, LIU Sen1, GAO Chao-hui1, CHEN Xiao-song1, GUO Yang-hong2, WANG En-si3, FANG Xue-xun1 and WANG Ji-dong1*   

  1. 1. College of Life Science;
    2. College of Chemistry;
    3. School of Pharmaceutical Sciences, Jilin University, Changchun 130021, P. R. China
  • Received:2009-05-25 Revised:2009-10-21 Online:2010-05-25 Published:2010-07-27
  • Contact: WANG Ji-dong. E-mail: deepseasoncn@yahoo.com.cn
  • Supported by:

    Supported by the National Natural Science Foundation of China(No.30371675) and the Foundation of Science & Technology Department of Jilin Province, China (No.20040543).

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摘要：

Many degenerative diseases caused by uncontrolled cell death can be intervened pharmaceutically through inhibiting caspase-3 activity that leads to cell apoptosis. Here is presented the discovery of rosolic acid and phenolphthalein methyl ester, which both belong to fuchsone derivatives, as novel and potent nonpeptide inhibitors of caspase-3. They show high inhibitory potency against caspase-3 in vitro(IC50=0.28 and 0.13 μmol/L). Molecular modeling study provided further an insight into the interaction of phenolphthalein methyl ester with activated caspase-3. The structures of the present small-molecule caspase-3 inhibitors are different from the structures of known caspase-3 inhibitors, so the inhibitors were likely to provide some information for the discovery of anti-caspase-3 inhibitors.

关键词: Caspase-3; Inhibitor; Fuchsone derivative; Docking simulation

Abstract:

Many degenerative diseases caused by uncontrolled cell death can be intervened pharmaceutically through inhibiting caspase-3 activity that leads to cell apoptosis. Here is presented the discovery of rosolic acid and phenolphthalein methyl ester, which both belong to fuchsone derivatives, as novel and potent nonpeptide inhibitors of caspase-3. They show high inhibitory potency against caspase-3 in vitro(IC50=0.28 and 0.13 μmol/L). Molecular modeling study provided further an insight into the interaction of phenolphthalein methyl ester with activated caspase-3. The structures of the present small-molecule caspase-3 inhibitors are different from the structures of known caspase-3 inhibitors, so the inhibitors were likely to provide some information for the discovery of anti-caspase-3 inhibitors.

Key words: Caspase-3; Inhibitor; Fuchsone derivative; Docking simulation