Acta Chimica Sinica ›› 2012, Vol. 70 ›› Issue (11): 1295-1303.DOI: 10.6023/A1202031 Previous Articles     Next Articles

Full Papers

具有抗癌活性的新型硒杂环化合物的合成及其与牛血清蛋白的相互作用

罗懿a, 陈填烽a, 黄晓纯a, 王弋a, 黄荫成b, 郑文杰a   

  1. a 暨南大学化学系 广州510632;
    b 香港中文大学生命科学学院 香港沙田
  • 收稿日期:2012-02-03 修回日期:2012-02-14 出版日期:2012-06-14 发布日期:2012-02-14
  • 通讯作者: 陈填烽, 郑文杰 E-mail:tchentf@jnu.edu.cn, tzhwj@jnu.edu.cn
  • 基金资助:

    教育部新世纪优秀人才支持计划(NCET 10-0119), 国家自然科学基金项目(Nos. 21071062, 20901030)和广东省科技攻关项目(No. 2008A030201020).

Synthesis, Anticancer Activity of a Novel Selenadiazole Derivative and Its Interaction with Bovine Serum Albumin

Luo Yia, Chen Tianfenga, Huang Xiaochuna, Wang Yia, Wong Yumshingb, Zheng Wenjiea   

  1. a Department of Chemistry, Jinan University, Guangzhou 510632;
    b School of Life Sciences, The Chinese University of Hong Kong, Hong Kong
  • Received:2012-02-03 Revised:2012-02-14 Online:2012-06-14 Published:2012-02-14
  • Supported by:

    Project supported by New Century Excellent Talents in University (NCET 10-0119), the National Natural Science Foundation of China (Nos. 21071062 and 20901030), Key Project of Science and Technology Department of Guangdong Province (No. 2008A030201020).

A novel selenadiazol derivative (BSBD) has been synthesized, characterized and evaluated for its anticancer activity. The in vitro anticancer activities of BSBD were screened by MTT assay against various cancer cell lines and it was found that BSBD could effectively inhibit cancer cell growth, especially for Nuero-2a neuroblastoma cells. Further investigation on the action mode showed that BSBD could induce Sub-G1 peak accumulation, chromatin condensation and the formation of apoptotic body in a dose-dependent manner in cancer cells, indicating that induction of apoptosis is the main mechanism accounting for the action of BSBD. Moreover the interaction between BSBD and bovine serum albumin (BSA) was investigated by UV-Vis, fluorescence and circular dichroism spectrometry and FTIR. The binding constants, number of binding sites and type of binding force were calculated by applying the equation of site-binding model and thermodynamic equations. The results of UV-Vis, FTIR and circular dichroism spectrometry revealed that the major interaction mode between BSA and BSBD was static quenching, due to hydrogen bonding and van der Waals force. The results of spectroscopic characterization showed BSBD altered the chemical structure and conformation of BSA.

Key words: selenadiazole derivative, anticancer activities, bovine serum albumin, interation, fluorescence quenching