betadex and kaempferol

Fisetin,quercetin and kaempferol are among the important representatives of flavonols, biological active phytocomounds, with low water solubility.. To evaluate the antimicrobial effect, respectively the antiproliferative and pro apoptotic activity on the B164A5 murine melanoma cell line of pure flavonols and their beta cyclodextrins complexes.. Incorporation of fisetin, quercetin and kaempferol in beta cyclodextrins was proved by scanning electron microscopy (SEM), differencial scanning calorimetry (DSC) and X-ray powder diffraction (XRPD). Pure compounds and their complexes were tested for antiproliferative (MTT) and pro-apoptotic activity (Annexin V-PI) on the B164A5 murine melanoma cell line and for the antimicrobial properties (Disk Diffusion Method) on the selected strains.. The phytocompounds presented in a different manner in vitro chemopreventive activity against B164A5 murine melanoma cell line and weak antimicrobial effect.. The three flavonols: fisetin, quercetin and kaempferol were successfully incorporated in beta-cyclodextrin (BCD) and hydroxylpropyl-beta-cyclodextrin (HPBCD). Incorporation in beta cyclodextrins had a mix effect on the biological activity conducing to decrease, increase or consistent effect compared to pure phytocompound, depending on the screened process and on the chosen combination.

Topics: Animals; Anti-Bacterial Agents; Antineoplastic Agents; Apoptosis; Bacteria; beta-Cyclodextrins; Cell Proliferation; Cell Survival; Chemistry, Physical; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Flavonoids; Flavonols; Kaempferols; Mice; Microbial Sensitivity Tests; Molecular Structure; Quercetin; Structure-Activity Relationship; Tumor Cells, Cultured

The utilization of kaempferol and its glycosides in food and pharmaceutical industries could be improved by the formation of inclusion complexes with cyclodextrins at different pH. This study explores the complexation of kaempferol-4'-glucoside with sulfobutyl ether-β-cyclodextrin (SBE-β-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD), and methylated-β-cyclodextrin (M-β-CD) in phosphate buffer solutions of different pH using isothermal titration calorimetry, UV-vis absorption and proton nuclear magnetic resonance spectroscopy at 298.2 K. Experimental results showed that kaempferol-4'-glucoside binds with the three β- cyclodextrins in the same 1:1 stoichiometry. The rank order of stability constants is SBE-β-CD > HP-β-CD > M-β-CD at the same pH level and pH 6.0 > pH 7.4 > pH 9.0 for the same cyclodextrin. The binding of kaempferol-4'-glucoside with the three β-cyclodextrin derivatives is synergistically driven by enthalpy and entropy at pH 6.0 and enthalpy-driven at pH 7.4 and 9.0. The possible inclusion mode was that in the cavity of β-CD is included the planar benzopyranic-4-one part of the kaempferol-4'-glucoside.

Topics: beta-Cyclodextrins; Calorimetry; Entropy; Glucosides; Hydrogen-Ion Concentration; Kaempferols; Molecular Structure; Solubility; Spectrum Analysis

A method was proposed to determine kaempferol and quercetin in Hippophae rhamnoides L medicinal preparation xindakang tablet by β-cyclodextrin modified micellar electrokinetic capillary chromatography. Under the optimized conditions: buffer solution of 20 mmol/L Na(2)B(4)O(7)-KH(2)PO(4) (pH 9.0)-20mmol/L SDS-6mmol/L β-CD-5%(v/v) MeCN, applied voltage of 16 kV and injection time of 8s, the two analytes were separated well within 10 minutes. The calibration was linear in the 0.02-0.80 and 0.02-0.70 mg/mL range for kaempferol and quercetin, respectively. The reproducibility based on migration time and peak height were 0.47% and1.87% for kaempferol, 0.55% and 2.02% for quercetin. The detection limits based on three times noise were 0.010 mg/mL and 0.008 mg/mL for kaempferol and quercetin, respectively. The developed method was utilized to analyze real samples and running recovery experiments with satisfactory results.

Topics: beta-Cyclodextrins; Chromatography, Micellar Electrokinetic Capillary; Kaempferols; Medicine, Chinese Traditional; Quercetin; Tablets