aspalathin and dihydrochalcone

Aspalathin is a

Topics: Antioxidants; Aspalathus; Chalcones; Dietary Supplements; Herb-Drug Interactions; Metabolic Syndrome; Oxidative Stress; Teas, Herbal

The bioactive hydrophilic dihydrochalcone, aspalathin, has poor stability and bioavailability hampering its use in functional food ingredients with standardised aspalathin content. The aim of the study was to produce nanoparticles with controlled release to overcome these obstacles. Nanoencapsulation was investigated using both natural (chitosan and lecithin) and synthetic (poly(lactide-co-glycolide) and Eudragit S100® (ES100)) polymers by suitable conventional methods and electrospraying for all polymers. All polymer-method combinations produced particles smaller than 1.1 µm. Electrospraying produced more favourable results than conventional methods for the synthetic polymers, resulting in spherical particles with higher (p < 0.05) encapsulation efficiencies (>50%) and loading capacities (>10%). Opposite trends were observed for natural polymers. An in vitro release study revealed biphasic aspalathin release profiles at pH 7.4 with ES100 electrosprayed nanoparticles having the slowest (p < 0.05) release rate (1.67 h

Topics: Aspalathus; Calorimetry, Differential Scanning; Chalcones; Chitosan; Hydrogen-Ion Concentration; Liposomes; Nanoparticles; Polyglactin 910; Spectroscopy, Fourier Transform Infrared

Metformin is the first line therapy of type 2 diabetics, but continued reduction of their life expectancy warrants further investigation into alternative treatment strategies. This study reports on the combinational use of metformin with aspalathin, a C-glucosyl dihydrochalcone with known glucose lowering and antioxidant properties, as an effective hypoglycemic therapy in a type 2 diabetic (db/db) mouse model. When tested as a monotherapy, a low dose of aspalathin (13 mg/kg) showed no effect, while a high dose (130 mg/kg) has already displayed a better potential than metformin in protecting against diabetes associated symptoms in db/db mice. Thus, it remains of interest to determine whether this dihydrochalcone can improve the efficacy of metformin. The results showed that this combination therapy was more effective than the use of metformin as a monotherapy in ameliorating diabetes associated symptoms, including abnormal raised fasting plasma glucose levels, impaired glucose tolerance, as well as excessively increased body weights and fat content. The treated mice also had reduced food and water consumption when compared to untreated controls, with a pronounced effect evident in the last week of treatment. Therefore, this study supports further investigations into the ameliorative effect of combination therapy of metformin and aspalathin against diabetes associated symptoms.

Topics: Animals; Aspalathus; Chalcones; Diabetes Mellitus, Type 2; Drug Synergism; Flavonoids; Hypoglycemic Agents; Male; Metformin; Mice; Mice, Inbred C57BL; Mice, Transgenic

Aspalathin and nothofagin are typical ingredients of unfermented rooibos (Krafczyk, N.; Glomb, M. A. J. Agric. Food Chem. 2008, 56, 3368). During oxidation these dihydrochalcones were degraded to higher molecular weight browning products under aerated and nonenzymatic conditions. In the early stages of browning reactions aspalathin formed two dimers. These two compounds were unequivocally established as atropisomers stemming from oxidative A to B ring coupling. Multilayer countercurrent chromatography (MLCCC) and preparative high-performance liquid chromatography (HPLC) were applied to obtain pure substances. The purity and identity of isolated dimers were confirmed by different NMR experiments, HPLC-DAD-MS, and HR-MS. In parallel to the formation of chromophores during the fermentation of black tea, the formation of aspalathin dimers implies an important mechanistic channel for the generation of color during the processing of rooibos.

Topics: Aspalathus; Chalcones; Dimerization; Oxidation-Reduction; Plant Extracts

FT-Raman spectroscopy was used for the first time for in situ identification of aspalathin and quantification of the dihyrochalcones in dried, green rooibos (Aspalathus linearis). With the support of two-dimensional correlation spectroscopy, characteristic key bands of aspalathin, the main flavonoid and antioxidant occurring in rooibos, were localized and identified in the spectra obtained from various plant samples. Application of Raman mapping revealed the spatial distribution of this valuable dihydrochalcone within the intact dried leaves. Based on the spectral data and reference HPLC values, reliable multivariate calibration models were developed for quantification of aspalathin, nothofagin, and the combined dihydrochalcone contents of dried, green rooibos.

Topics: Antioxidants; Aspalathus; Calibration; Carotenoids; Chalcones; Chromatography, High Pressure Liquid; Flavonoids; Lignin; Models, Biological; Plant Leaves; Spectrum Analysis, Raman