Pal Kaushik, Mallick Suman, Koner Apurba L
Department of Chemistry, Indian Institute of Science Education and Research Bhopal, Bhopal, India.
Phys Chem Chem Phys. 2015 Jun 28;17(24):16015-22. doi: 10.1039/c5cp01696g. Epub 2015 Jun 1.
Host-guest complexation of dapoxyl sodium sulphonate (DSS), an intramolecular charge transfer dye with water-soluble and non-toxic macrocycle γ-cyclodextrin (γ-CD), has been investigated in a wide pH range. Steady-state absorption, fluorescence and time-resolved fluorescence measurements confirm the positioning of DSS into the hydrophobic cavity of γ-CD. A large fluorescence enhancement ca. 30 times, due to 1 : 2 complex formation and host-assisted guest-protonation have been utilised for developing a method for the utilisation of CD based drug-delivery applications. A simple fluorescence-displacement based approach is implemented at physiological pH for the assessment of binding strength of pharmaceutically useful small drug molecules (ibuprofen, paracetamol, methyl salicylate, salicylic acid, aspirin, and piroxicam) and six important antibiotic drugs (resazurin, thiamphenicol, chloramphenicol, ampicillin, kanamycin, and sorbic acid) with γ-CD.
已在很宽的pH范围内研究了分子内电荷转移染料达波昔磺酸钠（DSS）与水溶性无毒大环γ-环糊精（γ-CD）的主客体络合作用。稳态吸收、荧光和时间分辨荧光测量证实了DSS位于γ-CD的疏水腔内。由于形成1:2络合物和主体辅助客体质子化，荧光大幅增强约30倍，已被用于开发一种基于环糊精的药物递送应用方法。在生理pH下采用一种简单的基于荧光位移的方法来评估药学上有用的小药物分子（布洛芬、对乙酰氨基酚、水杨酸甲酯、水杨酸、阿司匹林和吡罗昔康）以及六种重要抗生素药物（刃天青、甲砜霉素、氯霉素、氨苄青霉素、卡那霉素和山梨酸）与γ-CD的结合强度。
