Format

Send to

Choose Destination
Carbohydr Polym. 2013 Aug 14;97(1):196-202. doi: 10.1016/j.carbpol.2013.04.066. Epub 2013 May 2.

Complexation of fisetin with novel cyclosophoroase dimer to improve solubility and bioavailability.

Author information

1
Department of Bioscience and Biotechnology, Bio/Molecular Informatics Center & Institute for Ubiquitous Information Technology and Applications (CBRU), Konkuk University, Seoul 143-701, South Korea.

Abstract

Rhizobium species produce cyclosophoraose (Cys), which is an unbranched cyclic β-(1,2)-glucan. We synthesized novel cationic cyclosophoraose dimer (Cys dimer) and its structure was confirmed via NMR spectroscopy and MALDI-TOF mass spectrometry analysis. In this study, we investigated the complexation of hardly soluble drug fisetin (3,3',4',7-tetrahydroxyflavone) with Cys dimer to improve the solubility of fisetin, and its solubility was increased up to 6.5-fold. The solubility of fisetin with Cys dimer showed 2.4-fold better than with β-cyclodextrin. The fisetin-Cys dimer complex was characterized by using, phase solubility diagram, 2D NMR, FT-IR spectroscopy, SEM, DSC analysis and molecular modeling. Through the molecular docking simulations, complexation ability of fisetin with host molecules were in the following order: Cys dimer>Cys monomer>β-CD. The fisetin-Cys dimer complex showed also higher cytotoxicity to HeLa cells than free fisetin, indicating that the Cys dimer to improve bioavailability of fisetin.

PMID:
23769537
DOI:
10.1016/j.carbpol.2013.04.066
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center