Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (11): 2317-2323.DOI: 10.6023/cjoc201403020 Previous Articles     Next Articles



郭改英a, 唐青b, 黄英b, 陶朱a, 薛赛凤a, 祝黔江a   

  1. a 贵州大学贵州省大环化学及超分子化学重点实验室 贵阳 550025;
    b 贵州大学生化工程中心 贵阳 550025
  • 收稿日期:2014-03-07 修回日期:2014-05-14 发布日期:2014-07-01
  • 通讯作者: 黄英,;陶朱,;
  • 基金资助:


Influences on Shift of pKa, Solubility and Antifungal Activity ofFuberidazole by Inclusion Complexation with Cucurbit[n]urils

Guo Gaiyinga, Tang Qingb, Huang Yingb, Tao Zhua, Xue Saifenga, Zhu Qianjianga   

  1. a Key Laboratory of Macrocyclic and Supramolecular Chemistry of Guizhou Province, Guiyang 550025;
    b Biochemical Engineering Center of Guizhou Province, Guiyang 550025
  • Received:2014-03-07 Revised:2014-05-14 Published:2014-07-01
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.21202026), the Ministry of Education Chuihui Plan (No.Z2011034), the Department of International Cooperation Projects of Guizhou Province (No.[2012]7003), and the Talent Cultivation Project of Guizhou Province (No.2012154).

Interaction between cucurbit[n]uril (Q[n], n=6, 7, 8) and fuberidazole (FBZ) in HCl solution at pH 2.5 was investigated by UV-Vis spectroscopy, ITC, 1H NMR spectroscopy. The shift of pKa and bioactivities against Fusarium graminearum about fuberidazole and its host-guest inclusion complexes were discussed. The results showed that the inclusion complexes between cucurbit[n]urils and fuberidazole were formed, and the corresponding pKa of complexes have shifted. In addition, complexation by Q[n] (n=6, 7, 8) has proven to cause solubility enhancement. The activity experimental results showed that complexation of fuberidazole with Q[n] (n=6, 7) recedes activity against Fusarium graminearum while with Q[8] enhances the activity against Fusarium graminearum in vivo.

Key words: cucurbit[n]urils, fuberidazole, spectroscopy, ITC, bioactivities