八元瓜环与常山碱的相互作用模式

Interaction Mode Between Q[8] and Feb

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. 20×10^4L/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。

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).