| 七元瓜环对阿糖胞苷稳定性的影响 |
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| 引用本文： | 黄英,宋桂先,唐青,王娟,陶朱,薛赛凤,张建新.七元瓜环对阿糖胞苷稳定性的影响[J].高等学校化学学报,2014,35(6):1224-1228. |
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| 作者姓名： | 黄英 宋桂先 唐青 王娟 陶朱 薛赛凤 张建新 |
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| 作者单位： | 1. 贵州大学西南药用生物资源教育部工程研究中心, 2. 贵州省大环化学与超分子化学重点实验室,3. 贵州省中国科学院天然产物化学重点实验室, 贵阳 550025 |
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| 基金项目： | 国家自然科学基金(批准号:21202026);国家重大科学仪器设备开发专项项目(批准号:2011YQ120035);贵州省科技厅国际合作项目(批准号:黔科合外G字[2012]7003号);教育部春晖计划(批准号:Z2011034);贵州省英才培育项目(批准号:2012154)资助~~ |
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| 摘 要： | 研究了七元瓜环(Q7])与抗癌药物阿糖胞苷(Ara-C)的不同质子化存在形式之间的超分子相互作用, 探讨了超分子包合作用对药物电离平衡常数及药物稳定性的影响. 结果表明, Q7]使得Ara-C的pKa降低了约0.3个单位, Q7]与Ara-C的2种存在形式(Ara-C+及Ara-C)均可形成1∶1的主客体包结配合物, Ara-C以其嘧啶环进入Q7]空腔, 而核糖环位于瓜环端口发生相互作用; Q7]与Ara-C作用后对药物起到保护性载体的作用, 从而提高了药物的稳定性.
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| 关 键 词： | 阿糖胞苷 七元瓜环 主客体配合物 稳定性 |
| 收稿时间： | 2013-09-30 |
Encapsulation of Cytarabine in Cucurbit[7]uril and Its Effects on Stability of the Drug† |
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| HUANG Ying,SONG Guixian,TANG Qing,WANG Juan,TAO Zhu,XUE Saifeng,ZHANG Jianxin.Encapsulation of Cytarabine in Cucurbit[7]uril and Its Effects on Stability of the Drug†[J].Chemical Research In Chinese Universities,2014,35(6):1224-1228. |
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| Authors: | HUANG Ying SONG Guixian TANG Qing WANG Juan TAO Zhu XUE Saifeng ZHANG Jianxin |
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| Institution: | 1. The Engineering and Research Center for Southwest Bio-Pharmaceutical Resources, Ministry of Education,2. Key Laboratory of Macrocyclic and Supramolecular Chemistry of Guizhou Province,3. The Key Laboratory of Chemistry for Nature Products of Gui Zhou Province and Chinese Academy of Science,Guizhou University, Guiyang 550025, China |
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| Abstract: | The interaction of cucurbit7]uril(Q7]) with cytarabine(Ara-C) in different proton forms were studied by ultraviolet absorption spectroscopy and 1H NMR technique in details. Complexation by Q7] has also been investigated to cause pKa shifts and stability of drug. The results showed that Q7] encapsulated the Ara-C and shifted its pKa value by down to 0.3 units. Ara-C in different proton forms with Q7] informed 1∶1 inclusion complexes, and the formation constants were (9.48±0.29)×103 L/mol and (6.30±0.04)×103 L/mol for the Q7]-Ara-C+ system and Q7]-Ara-C system, respectively. Moreover, The formation of inclusion complexes between Q7] with Ara-C was confirmed by 1H NMR, the pyrimidine moiety of Ara-C were entrapped in the cavity of the host and the D-ribose ring was likely located at the outside cucurbituril cavity. In addition, stability studies were investigated by initial uniform rate experiment. The results revealed that complexation of Ara-C with Q7] offers a major improvement in drug stability. |
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| Keywords: | Cytarabine Cucurbit[7]uril Inclusion complex Stability |
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