Mechanochemistry Assisted Extraction Of Active Compounds From Sophora Flavescens And Solubilization System Development

The traditional solvent-heating extraction method has the disadvantages of low extraction efficiency,the use of large amount of organic solvent,and poor selectivity.Mechanochemistry as a new auxiliary mean of extraction method,can efficiently break the cell wall and facilitate solvent pass through the cell to dissolve the active components.Solid state reactions in cell promoted by mechanical force can increase water solubility of hydrophobic components,and therefore reduce the use of organic solvents.The development of the solubilization system of plant active ingredients by mechanochemistry can improve the dissolution or dissolution,which will greatly improve the application scope and economic value of the extracts and reduce the waste of the active ingredients.In this dissertation,mechanochemistry as the characteristics was applied to assisted-extract active components from Sophora flavescens Ait.(SFA)and develop the solubilization system of hydrophobic flavonoids and curcumin.The structure of this dissertation is divided into three parts:(1)summary of effective components in SFA and mechanochemical technology;(2)mechanochemical-assisted extraction and separation of effective components from SFA;(3)the development of mechanochemistry in preparation of solubilization system of hydrophobic flavonoids and curcumin.In the first part,pharmacological activity of SFA and its effective components were summarized.The development history,characteristics and application fields of mechanochemistry were briefly introduced.The principle and application of mechanochemical technology in extraction of effective components from plant material and in the development of drug preparations were emphasized.In the second part,active compounds were mechanochemical-assited extracted from SFA,achieving the comprehensive utilization of compounds in SFA.Alkaline reagent magnesium carbonate were added during milling process,followed by using water as solvent to extract alkaloids,flavonoids,polysaccharide,affording the yields of 36.77mg/g,35.17 mg/g,114.25 mg/g,respectively.The main component in flavonoid extracts including Kushenol,Kurarinone,and Kurarinol I/N were identified by HPLC/MS/MS.Compared with the traditional extraction method,mechanochemical-assited extraction method could decrease the use amount of organic solvent,enhance extraction efficiency and selectivity,which was green and environmental friendly.In the third chapter,polysaccharide were further purified by DEAE-52 cellulose column and gel column to obtain four polysaccharide fragments(SF1,SF2,SF3,SF4)with different molecular weights,which were all acidic polysaccharides,mainly composed of rhamnose,xylose,mannose,arabinose,glucose and galactose with different proportions.Antioxidant experiment in vitro demonstrated that SF4 had significant scavenging effect on ABTS radical,DPPH radical and superoxide anion radical,while SF3 had good scavenging effect on hydroxyl radical.The results of cellular immunity test in vitro showed that the four polysaccharide fragments had no cytotoxicity to macrophages,activated macrophages to produce nitric oxide and promoted the proliferation of spleen cells.In the third part,it was firstly developed a mechanochemical-promoted solubilization system for flavonoids.It was performed by analysis the effect of the pH value of the solution and various inorganic alkali and hydrophilic carrier on the solubilization of flavonoids,and finally the optimal solubilizing carrier(medium)was screened.In the second part of the fourth chapter,curcumin was selected as the natural pure phenol to investigate the solubilization system because of its cheap price and easy obtaining.Through the optimization of the mechanical grinding conditions and the selection of the excipients,polysaccharide arabinogalactane and sodium glycyrrhizinate were chosed as the optimal excipients.Differential scanning calorimetry(DSC),X-ray diffraction(XRD),scanning electron microscope(SEM),Fourier-transformed infrared spectra(FTIR),1H-NMR,and transmission electron microscopy(TEM)were applied to characterization the physicochemical properties and mechanism of solubilization system.The solubility of curcumin solubilizing system was increased by nearly 400 times as compared to free curcumin.Curcumin solubilizing system showed an increased permeability in vitro parallel artificial membrane permeability assay.Animal experiments demonstraed that bioavailability of curcumin solubilizing system was increased by 11.3 times compared to free curcumin.