Abstract: 3-butyryl-8-methoxy-4-(2-ethylphenylamino) quinoline(SK&F 96067) has been used as an H⁺-K⁺ ATPase inhibitor. It is insoluble in water. The formation of the inclusion complex between drug SK&F 96067 and β-CD was studied by UV absorption, fluorescence and ¹H-NMR spectroscopy. In the aqueous environment a clear isosestic point was observed in the absorption spectra. The fluorescence intensity of SK&F 96067 increased as the concentration of β-CD increased. Continuous variation plot by fluorescence study suggested that 1∶1(guest∶host) stoichiometric complex was formed in the solution. The spectral analysis of ¹H-NMR measurement showed that the signals of the quinoline protons of SK&F 96067 were shifted downfield, resulting from the interaction of β-CD with quinoline ring of SK&F 96067.

Key words: 3-butyryl-8-methoxy-4-(2-ethylphenylamino) quinoline (SK&F 96067), β-cyclodextrin

摘要： 3-丁酰基-8-甲氧基-4-(2-甲基苯基氨基)喹啉(SK&F 96067)是新合成的H⁺-K⁺-ATP酶抑制剂，它难溶于水。通过紫外吸收光谱、分子荧光光谱和¹H-NMR的方法研究该药物分子与β-环糊精(β-CD)之间包合物的形成。研究发现在水环境中该药物分子的紫外吸收光谱有明显的等吸光度点；而且其荧光强度随着β-CD浓度的增大而增强，两者的拟合结果表明在水溶液中该药物分子能够与β-CD形成1∶1(客体∶主体)的包合物；¹H-NMR的谱图显示该药物分子喹啉环上的质子信号向低场迁移，这是由于其喹啉环部分地进入了β-CD疏水腔的结果。

关键词: 3-丁酰基-8-甲氧基-4-(2-甲基苯基氨基)喹啉(SK&F96067), β-环糊精(β-CD), 包合物, 分子荧光, ¹H-NMR