Preliminary Study On The Extraction,purification,and Biological Activity And Delivery System Construction Of Gingerols

Ginger is widely cultured in China and serves as the representative of China medicine and food homologous.Gingerols(GRs)is the main active component of ginger that shows biological activities and pharmacologic properties.Despite the GRs researches has been focus over the evidences for a number of biological effects,there are few researches on the efficient isolation and purification,construction of delivery system and other application research.Therefore,it is imperative to perform research for development and utilization of GRs.In the study,non-thermal pulsed electric field technology(PEF)-assisted method was applied to enhance the extraction processes,giving higher yields and better extract quality.After extraction,further enrichment and purification with macroporous resin was carried out to meet the purity demands.The primary gingerols,6-gingerols,8-gingerols and 10-gingerols,were investigated with the antioxidant capacity and the inhibition on the activity of xanthine oxidase(XOD)activity,a key enzyme catalyzing xanthine to uric acid and finally causing gout.The work has the potential to provide guidance for the development of new antioxidant and anti-gout drugs and functional foods.Finally,an efficient drug delivery system were prepared via the bovine serum albumin(BSA),for enhancing the water solubility and improving the bioavailability of GRs.And it could be a promising dosage form to broaden the application prospect of GRs.The main research conclusions are as follows:Various extraction methods were evaluated and compared with the yield of GRs,PEF was selected as the most efficient extraction technology with the yield of 13.36 mg/g.Optimization of major variations was done by single-factors and the response surfaces design.And the modeled optimal conditions were pulse width 9?s,pulse time 22,and electric field intensity 2.0 k V/cm,with the corresponding yield being 14.68±0.46 mg/g.There was around70.13%increase in the yield of GRs than the conventional organic solvents methods.AB-8 resin exhibited the best adsorption and desorption capacity for GRs among five macroporous resins.The kinetics and isotherms of adsorption describe a multi-molecular layer adsorption behavior governing the chemical process,with the simulated equilibrium adsorption capacity of 37.83 mg/g.Three various factors on the influence of desorption was investigated to obtain the optimal conditions:p H 6.0,the volume alcohol 80%and the elation time 3.0 h.After the treatment at optimal parameters of absorption and desorption process,the purity of 6-gingerols,8-gingerols and 10-gingerols increased 2.7 times,4.3 times,and 5.48times increase,respectively.The antioxidant and XOD enzyme inhibitory activities were determined,10-gingerol exhibited the strongest activities,with IC₅₀ values of 0.349 m M for DPPH,0.065 m M for ABTS,and 6.88?M for XOD.The kinetic analysis manifested that GRs were reversible mixed-type competitive inhibitor with two inhibition paths lowering uric acid,one was the bind with free enzymes and the other one was combination with enzyme-substrate complexes.A novel GRs delivery system was fabricated by the BSA nanoparticles at a 1:4(BSA:GRs),with the drug entrapment efficiency of BSA-6G,BSA-8G and BSA-10G at 13.72±0.39 mg/g?15.70±0.29 mg/g?18.70±0.58 mg/g,respectively.The unloading efficiency of BSA to 10G was the best.The increasement of particle size(from 449.4±1.89to 743.8±4.31 nm)and PDI(from 0.269±0.013 to 0.387±0.023),the decrease of surface hydrophobic(591.2±0.7 to 483.85±0.9)of nanoparticles after GRs incorporation and the secondary structure of protein contracted.The FTIR and TG results indicated that GRs were bound to BSA.The bind mode and behavior were investigated by fluorescence quenching measurements and docking studies.The quenching mechanism(BSA/GRs)was confirmed as the static quenching with the medium binding affinity and the binding constant(K_a)was0.594-6.853 mol/L.The interactions actions were occurred mainly in subdomain?A of BSA and the hydrophobic interaction played major roles accompanied a few hydrogen bond.The solubility,antioxidant activity and stability of GRs were improved after encapsulation in the BSA nanoparticles.The most significant difference affected on the property of 10-gingerol:the solubility increased by 23.50 times,the antioxidant activity improved by more than 30%,and the thermal stability increased from 5.06%to 16.45%at80°C,the digestion retention rate reached 69.71%.Therefore,BSA is an effective delivery carrier for GRs,which provides the theoretical basis for the development and application of GRs.