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化学学报
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化学学报 ›› 2011, Vol. 69 ›› Issue (12): 1431-1437. 上一篇    下一篇

研究论文

七、八元瓜环对抗癌药物苯丁酸氮芥稳定性和溶解度的影响研究

董南*,1,2，王秀林2，盘金品2，陶朱1,2   

  1. (1贵州省大环化学及超分子化学重点实验室 贵州大学 贵阳 550025)
    (2贵州大学化学与化工学院 贵阳 550025)
  • 投稿日期:2010-10-13 修回日期:2011-01-05 发布日期:2011-02-24
  • 通讯作者: 董南 E-mail:sci.ldong@gzu.edu.cn
  • 基金资助:

    贵州省省长基金资助;贵州省自然科学基金资助项目;贵州大学人才引进项目;国家自然科学基金项目

Influence of Cucurbit(n＝7,8)uril on the Solubility and Stability of Chlorambucil

Dong Nan*,1,2 Wang Xiulin2 Pan Jinpin2 Tao Zhu1,2   

  1. (1 Key Laboratory of Macrocyclic and Supramolecular Chemistry of Guizhou Province, Guizhou University, Guiyang 550025)
    (2 School of Chemistry and Chemical Engineering, Guizhou University, Guiyang 550025)
  • Received:2010-10-13 Revised:2011-01-05 Published:2011-02-24

PDF

1595

被引次数

15

利用高效液相色谱法考察七、八元瓜环对苯丁酸氮芥稳定性的影响. 结果表明在37 ℃, pH 2.0盐酸溶液中, 七元瓜环的浓度为2.0×10－4 mol•L－1时可使苯丁酸氮芥的稳定性提高近4倍, 而八元瓜环浓度为8.0×10－5 mol•L－1时可使苯丁酸氮芥的稳定性提高近15倍|相溶解度法的研究则证实在苯丁酸氮芥分解速度最低的条件下(3 ℃, pH 2.0盐酸溶液中), 1.0×10－3 mol•L－1浓度七元瓜环的存在可使苯丁酸氮芥的溶解度增加36倍, 八元瓜环浓度为1.0×10－4 mol• L－1时可增加6倍|通过紫外吸收光谱法考察了在不同pH条件下, 七、八元瓜环与苯丁酸氮芥的相互作用, 计算了瓜环与苯丁酸氮芥相互作用的稳定常数和作用比例, 并与动力学的结果进行了比较, 同时用核磁进一步验证了瓜环与苯丁酸氮芥的相互作用, 给出了可能的相互作用模式.

关键词: 七、八元瓜环, 苯丁酸氮芥, 稳定性, 溶解度, 相互作用

The effects of cucurbit(n＝7,8)uril (Q[7,8]) on the solubility and stability of chlorambucil (CHL) have been investigated. The results from high performance liquid chromatography indicated that in the presence of 2.0×10－4 mol•L－1 Q[7], there is a 4-fold increase in the stability of chlorambucil at 37 ℃, pH 2.0, while a greater 15-fold increase in the presence of 8.0×10－5 mol•L－1 Q[8] under same conditions. Aqueous solubility of CHL is increased more than 6-fold or 36-fold increase in the presence of 1.0×10－4 mol•L－1 Q[8] or 1.0×10－3 mol•L－1 Q[7] respectively under conditions where degradation is minimized (3 ℃, pH 2.0). Stability constants of the CHL complex with Q[7,8] were determined kinetically and spectrophotometrically under various experimental conditions assuming 1∶1 inclusion complex formation. 1H NMR further confirmed that Q[7,8] could form complexes with CHL and the possible interaction models were proposed.

Key words: cucurbit(n＝7,8)uril, chlorambucil, stability, aqueous solubility, interaction