Enhancing bio-availability of ß-naphthoflavone by supramolecular complexation with 6,6'-thiobis(methylene)-ß-cyclodextrin dimer.
Carbohydr Polym
; 151: 40-50, 2016 Oct 20.
Article
in En
| MEDLINE
| ID: mdl-27474541
ABSTRACT
The aryl hydrocarbon receptor (AhR) is a ligand activated transcriptional regulator, which governs key biological processes including detoxification of carcinogens. ß-Naphthoflavone (ß-NF) is a non-toxic flavonoid, and a potent AhR agonist. Thus, ß-NF can induce the representative detoxifying enzyme cytochrome P4501A1, thereby enhancing the detoxification potential. However, its low water solubility hampers the use. We found that supramolecular complexation of ß-NF with the synthetic 6,6'-thiobis(methylene)-ß-cyclodextrin (ß-CD-S) dimer significantly enhanced ß-NF's role as an AhR agonist. The water solubility of ß-NF was increased to 469 fold by effective supramolecular complexation with the ß-CD-S dimer, and caused significant induction of cytochrome P4501A1. Stable formation of the supramolecular complex of ß-NF with ß-CD-S-dimer was verified by various analyses. In summary, supramolecular complexation of ß-NF with ß-CD-S dimer greatly enhanced bio-availability of ß-NF as an AhR agonist. Our findings provide an easy, non-destructive, and alternative approach to enhance the bio-availability of therapeutics.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Beta-Naphthoflavone
/
Beta-Cyclodextrins
Type of study:
Prognostic_studies
Limits:
Humans
Language:
En
Journal:
Carbohydr Polym
Year:
2016
Document type:
Article
Publication country:
ENGLAND
/
ESCOCIA
/
GB
/
GREAT BRITAIN
/
INGLATERRA
/
REINO UNIDO
/
SCOTLAND
/
UK
/
UNITED KINGDOM