Studies On Mechanochemistry Extraction Of Flavone From Gynura Divaricata And In Vivo Solubilization Of Kaempferol

Gynura Divaricate（L.）DC.is a natural plant of the genus compositae and have various of pharmacological active ingredients.The rational development and utilization of flavonoids with high content in plant is of great significance.In this paper,we carried out the research on the mechanochemistry technology to assist the extraction of flavonoids,preparation of kaempferol soild dispertion free of organic reagent and pharmacological activity assay.The main research contents are as follows:1)The effects of the parameters of mechanical ball milling on the yield of flavonoids.The optimal extraction process was the ball grinding aid Na₂CO₃,ball milling time in 30 min,ball milling speed at 300 rpm and filling rate with 26.2%.Under the optimal conditions,the yield of total flavonoids and several representative flavonoids increased many times.2)The mechanical ball milling was used to preparation the soild dispertion of kaempferol.The formation of solid dispersion was confirmed by the experiments of SEM,XRD and DSC.The best solubility of the complexes was 184 times higher than original kaempferol and the dissolution rate increased by 2.2 times.After 90 days of the rapid storage test,the stability of KF-Na₂GA significant increased.3)Pharmacokinetic studies of the soild dispertion of KF have shown that through mechanochemistry processing,the absorption of kaempferol in vivo obviously improved,peak blood drug concentration increased 5 to7 times,peak time and the average residence time shortened,all of these phenomenons indicate the improvement of drug bioavailability.4)The pharmacological studies of the KF and its soild dispertion showed that the inhibitory activity of the glucose metabolism enzyme improved.Moreover,in the study of typeⅠdiabetes mice,the body metabolism,blood glucose level and glucose tolerance test in mice of KF soild dispertion groups are better than original KF group.Serum insulin levels,blood lipids,liver and kidney enzyme,oxidative indicators,and islet damage were also better than original KF group.This study provide a real research results and feasible ideas for the development and utilization of hypoglycemic activity of flavonoids and kaempferol with mechanochemistry technology.