期刊
CARBOHYDRATE RESEARCH
卷 418, 期 -, 页码 20-28出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.carres.2015.09.013
关键词
Fisetin; Cyclodextrins; Inclusion complex; Molecular modeling; Antitumor activity
资金
- Program for Changjiang Scholars and Innovative Research Team in University [IRT13095]
- National Natural Science Foundation of China [21442006, 21262043, 20902079]
Novel water-soluble inclusion complexes for fisetin (FIT) were developed by introducing beta-cyclodextrin (beta-CD) and gamma-CD. Properties of the obtained complexes, as well as the interactions between each component, were systematically investigated in both solution and solid states by means of ESI-MS, NMR, FTIR, XRD, DSC, SEM etc. All characterization information demonstrated that FIT/CDs inclusion complexes were formed, and exhibited different spectroscopic features and properties from FIT. A complex with 1: 1 stoichiometry of FIT and CDs was confirmed with Job's method. Meanwhile, as supported by molecular modeling calculations, we suggested that phenyl group (C ring) of FIT molecule was included in the CDs cavity from the wide side. Moreover, the water solubility of FIT/CDs was successfully improved from 2.8 mg/mL (in ethanol aqueous solution) to 4.5 mg/mL (FIT/beta-CD complex) and 7.8 mg/mL (FIT/gamma-CD complex), and higher thermal stability results were shown by thermal analysis for those complexes. Notably, the inclusion complexes displayed almost two times higher cytotoxicity compared to free FIT against Hela and MCF-7 cells. These results suggested that FIT/CDs complexes could be potentially useful in food industry and healthcare area. (C) 2015 Elsevier Ltd. All rights reserved.
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