高等学校化学学报 ›› 2020, Vol. 41 ›› Issue (2): 277-283.doi: 10.7503/cjcu20190380

• 有机化学 • 上一篇    下一篇

八元瓜环与常山碱的相互作用模式

蒋静1,2,陈晓丽3,黄亚励3,张奇龙1,3,*(),徐红3,*(),杨小生1   

  1. 1 贵州医科大学药用植物功效与利用国家重点实验室
    2 公共卫生学院环境污染与疾病监控教育部重点实验室
    3 基础医学院, 贵阳 550025
  • 收稿日期:2019-07-06 出版日期:2020-02-10 发布日期:2019-12-04
  • 通讯作者: 张奇龙,徐红 E-mail:gzuqlzhang@126.com;1738943269@qq.com
  • 基金资助:
    贵州省区域内一流学科建设项目(黔教科研发[2017]85号);贵州省科技计划项目(黔科合支撑[2019]2792号);贵州省科技计划项目(黔科合平台人才[2018]5779-14);贵州省苗医药重点实验室开放课题基金(黔苗医药K字[2017]023);大学生创新创业基金省级一般项目资助(2018520334)

Interaction Mode Between Q[8] and Feb

JIANG Jing1,2,CHEN Xiaoli3,HUANG Yali3,ZHANG Qilong1,3,*(),XU Hong3,*(),YANG Xiaosheng1   

  1. 1 State Key Laboratory of Functions and Applications of Medicinal Plants
    2 School of Public Health, Key Laboratory of Environmental Pollution Monitoring and Disease Control, Ministry of Education
    3 School of Basic Medical Science, Guizhou Medical University, Guiyang 550025, China
  • Received:2019-07-06 Online:2020-02-10 Published:2019-12-04
  • Contact: Qilong ZHANG,Hong XU E-mail:gzuqlzhang@126.com;1738943269@qq.com
  • Supported by:
    ? Supported by the First-Class Discipline Construction Project in Guizhou Province-Public Health and Preventive Medicine, China(黔教科研发[2017]85号);the Guizhou Provincial Natural Science Foundation, China(黔科合支撑[2019]2792号);the Guizhou Provincial Natural Science Foundation, China(黔科合平台人才[2018]5779-14);the Open Project Fund of Guizhou Provincial Miao Medicine Key Laboratory, China(黔苗医药K字[2017]023);the Provincial General Project of University Student Innovation and Entrepreneurship Fund, China(2018520334)

摘要:

利用紫外吸收光谱、 荧光光谱、 核磁共振氢谱及红外光谱等方法考察了八元瓜环(Q[8])对常山碱(Feb)的包结作用; 采用紫外吸收光谱法研究了Q[8]对Feb理化性质的影响及不同pH条件下Q[8]/Feb包合物溶液中Feb的释放及Q[8]/Feb包合物在人工肠液和人工胃液中的释放. 结果表明, 在pH=1.2的盐酸介质中, Q[8]与Feb可形成摩尔比1∶1的稳定主客体包合物, 结合常数为4.20×10 4 L/mol. 在pH=1.2(人工胃液的pH值)时, Feb可与Q[8]形成稳定包合物; 在pH=6.8(人工肠液的pH值)时, Q[8]/Feb包合物可释放出单纯的游离Feb. 因此, Q[8]可作为Feb的一种潜在药物载体为减轻Feb呕吐副反应提供借鉴.

关键词: 八元瓜环, 常山碱, 主客体包合物, 药物释放

Abstract:

Ultraviolet absorption spectroscopy, fluorescence spectroscopy, nuclear magnetic resonance spectroscopy, infrared spectroscopy and other methods were used to investigate the inclusion of Q[8] on Feb. The effect of Q[8] on the physicochemical properties of Feb was studied by UV absorption spectroscopy. The influences of Q[8] on the physicochemical properties of Feb and the release of Q[8]/Feb inclusion solution at different pH values and the release of Q[8]/Feb inclusion in artificial intestinal and gastric juice were studied by UV-Vis absorption spectroscopy. The results showed that Q[8] and Feb can form a stable host-guest complex with a molar ratio of 1∶1 in a hydrochloric acid medium with a pH of 1.2. The binding constant was 4.20×10 4 L/mol. At pH=1.2(artificial gastric juice), Feb can combined with Q[8], a stable complex can be formed. At pH=6.8(artificial intestinal juice), the Q[8]/Feb complex can release pure free Feb, which was stable in gastric juice and released in intestinal fluid. Q[8] may be used as a potential drug carrier for Feb to provide basic research data for alleviating the side effects of Feb vomiting, but the actual effect needs further experimental research. It may be due to the better solubility of Q[8] in acidic medium. The release of Q[8]/Feb solid inclusion compound in artificial gastric juice(pH=1.2) was greater than that of artificial intestinal juice(pH=6.8).

Key words: Q[8], Feb, Host-guest complex, Drug release