高等学校化学学报Issue(6)：1224-1228,5.DOI:10.7503/cjcu20130966
七元瓜环对阿糖胞苷稳定性的影响
Encapsulation of Cytarabine in Cucurbit[7]uril and Its Effects on Stability of the Drug
摘要
Abstract
The interaction of cucurbit[7]uril(Q[7]) with cytarabine(Ara-C) in different proton forms were studied by ultraviolet absorption spectroscopy and 1 H NMR technique in details. Complexation by Q[7] has also been investigated to cause pKa shifts and stability of drug. The results showed that Q[7] encapsulated the Ara-C and shifted its pKa value by down to 0. 3 units. Ara-C in different proton forms with Q[7] 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 Q[7]-Ara-C+ system and Q[7]-Ara-C system, respectively. Moreover, The formation of inclu-sion complexes between Q[7] with Ara-C was confirmed by 1 H 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 Q[7] offers a major improvement in drug stability.关键词
阿糖胞苷/七元瓜环/主客体配合物/稳定性Key words
Cytarabine/Cucurbit[7]uril/Inclusion complex/Stability分类
化学化工引用本文复制引用
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,(6):1224-1228,5.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)和贵州省英才培育项目(批准号:2012154)资助. Supported by the the National Natural Science Foundation of China(No.21202026), the National Major Scientific Instruments Development Project, China(No.2011YQ120035), the International Cooperation Projects of Science and Technology Agency of Guizhou Province, China(No.20127003), the “Chun-Hui” Fund of Ministry of Education, China( No. Z2011034) and the Young Talent Development Project of Guizhou Province, China(No.2012154) （批准号:21202026）
