10.6084/m9.figshare.3532262.v2
Jin Yan
Jin
Yan
Bin Tang
Bin
Tang
Di Wu
Di
Wu
Shanshan Li
Shanshan
Li
Kailin Xu
Kailin
Xu
Xiaoli Ma
Xiaoli
Ma
Qing Wang
Qing
Wang
Hui Li
Hui
Li
Synthesis and characterization of <i>β</i>-cyclodextrin/fraxinellone inclusion complex and its influence on interaction with human serum albumin
Taylor & Francis Group
2016
β-cyclodextrin
Fraxinellone
human serum albumin
inclusion complex
spectroscopy
2016-09-09 18:10:05
Journal contribution
https://tandf.figshare.com/articles/journal_contribution/Synthesis_and_characterization_of_-cyclodextrin_fraxinellone_inclusion_complex_and_its_influence_on_interaction_with_human_serum_albumin/3532262
<p>Aqueous solubility is one of the key determinants in developing new chemical entities as drugs. In this study, to improve the solubility of fraxinellone, a novel <i>β</i>-cyclodextrin/fraxinellone inclusion complex was prepared and characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, X-ray diffraction, and elemental analysis. Moreover, the influence of inclusion of small molecule by cyclodextrins on its binding with transporter in human body is essential for drug development. For the first time, we report the interaction of fraxinellone and its inclusion complex with human serum albumin. Fluorescence quenching of albumin by fraxinellone and its inclusion complex is a static process through complex formation. The results indicated that <i>β</i>-cyclodextrin did not affect the binding force and site of fraxinellone to the protein. Furthermore, circular dichroism showed that both fraxinellone and its inclusion complex induced a significant change in the secondary structure of human serum albumin.</p>