In order to expand the application in the medical field and enhance pharmacological effects, casein-myricetin nanomicelles were prepared by the self-assembly method and characterised by ultraviolet-visible spectroscopy and Fourier transform infrared spectroscopy. The parameters in self-assembly were optimised according to the factors of particle size, encapsulation yield, and drug loading. The result showed a pH of 5.5, a casein concentration of 2 mg/ml, a mass ratio of casein to myricetin of 8:1, ultrasonic power of 300 W, ultrasonic time of 5 min and ethanol volume of 7 ml were the optimal conditions. The situ cycle intestinal perfusion methods indicated that casein-myricetin nanomicelles can be more easily absorbed by small intestine than myricetin standard sample. Therefore, casein micelles are effective for improving the water solubility of myricetin.
Two anionic β-cyclodextrins as chiral selectors were successfully applied in the enantioseparation of N-methyl duloxetine, duloxetine, and fluoxetine by countercurrent chromatography. Sulfobutyl ether-β-cyclodextrin and carboxymethylβ-cyclodextrin showed opposite enantioselectivity for both duloxetine and N-methyl duloxetine enantiomers. Two biphasic solvent systems, n-hexane: 0.1 mol/L phosphate buffer pH 7.6 with 50 mmol/L of sulfobutyl ether-βcyclodextrin (1:1, v/v) and n-hexane: 0.1 mol/L phosphate buffer pH 7.2 with 50 mmol/L of carboxymethyl-β-cyclodextrin (1:1, v/v), were selected for Nmethyl duloxetine. Enantioseparation of duloxetine was achieved by recycling countercurrent chromatography using a solvent system composed of n-butyl acetate: 0.1 mol/L phosphate buffer pH 7.2 with 20 mmol/L of sulfobutyl ether-β-cyclodextrin or carboxymethyl-β-cyclodextrin (1:1, v/v). A solvent system composed of n-hexane: n-butyl acetate: 0.1 mol/L phosphate buffer pH 7.6 containing 20 mmol/L of sulfobutyl ether-β-cyclodextrin (6:4:10, v/v) was selected for enantioseparation of fluoxetine.
Hypoglycemic activity and mechanisms of myricetinMyricetin has been reported to have a wide variety of beneficial physiological functions. The present study was designed to investigate the mechanism of high purity myricetin, as a hypoglycemic functional component on high fat diet (HFD) fed streptozotocin (STZ) induced diabetic rats. Four-week antihyperglycemic effects of myricetin were assayed. The results showed that continuous administration of myricetin (50 and 200 mg/kg body weight) in HFD/STZ induced diabetic rats dose-dependently reduced the body serum glucose and insulin. Furthermore, administrations of myricetin significantly increased the expression of insulin receptor (InsR) and glucose transporter 4 (GLUT4) gene and increased the expression of glucose-6-phosphatase (G-6-Pase) and phosphoenolpyruvate carboxykinase (PEPCK) gene. Moreover, myricetin protected pancreatic tissue from HFD fed STZ induced apoptosis through regulation of Bcl-2 associated X (Bax) gene and B-cell lymphoma-2 (Bcl-2) gene. The experimental results show that myricetin has significant health benefits and can be explored as a potentially promising dietary supplement for auxiliary hypoglycemic.
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