Inclusion Complexes Of Scutellarin With Polyamine-β-cyclodextrin And Cationic β-cyclodextrin-polyrotaxanes:Synthesis,Characteriazation

Due to Cyclodextrins’ excellent properties and special structures,it is widely used in pharmaceutical,chemical and many other fields.Because of its special structure(external cavity is hydrophilic,hydrophobic cavity),which can make some hydrophobic drugs into cyclodextrins’ cavity to form the inclusion complexes,thus changing the physical and chemical properties of the drug molecules.Secondly,cyclodextrins inclusion linear polymers formed polyrotaxane,they not only increase the amount of drug loading function,but also be applied to gene therapy,which provides a new idea for the new gene carrier.This paper studies the inclusion behavior and genes carrier of cyclodextrins,on the one hand,we prepared scutellarin conclusion complexes and study their anticancer activity,on the other hand,by the cyclodextrin with polyether amine(PPG-NH2)to build the polyrotaxane,and a cationic modified polyrotaxane-containing alkyl group by embedding planar carrier structure,the performance of this system was studied.This paper specifically includes the following three parts:1.Several cyclodextrin derivatives were synthesized:mono-6-O-(p-tolysulfonyl)-β-cyclodextrin(TsO-βCD),mono-6-iodine-6-deoxy-β-cyclodextrin(I-βCD),mono-6-azido-6-deoxy-β-cyclodextrin(N3-βCD),mono(6-amino-6-deoxy)-β-cyclodextrin(NH2-PCD),mono(6-ethylenediamino-6-deoxy)-β-cyclodextrin(EN-βCD),mono(6-diethylenetriamino-6-deoxy)-β-cyclodextrin(DETA-βCD),mono(6-triethylenetetraamino-6-deoxy)-β-cyclodextrin(TETA-βCD).In the meantime,their structures were charactered by 1H NMR.2.The inclusion complexation behavior of scutellarin with four polyamine-modifiedβ-cyclodextrins(NH2-βCD,EN-βCD,DETA-βCD,TETA-PCD)has been investigated in both solution and the solid state.According to fluorescence spectrum and the calculation formula,we could obtain the inclusion ratio and stability constant(Ks);Moreover,the inclusion complexes were characterized by means of 1H NMR,XRD,TG and SEM.Through the analysis of 2D NMR and inclusion ratio,we speculated the possible inclusion mode.The measurement of solubility of the inclusion complexes in water ant its antitumor activity will be potentially useful for improving their bioavailability.3.We have successfully synthesized four polyrotaxanes(PR),including cationic polyrotaxanes(CPR)3 a,3b and scutellarin cationic polyrotaxanes(SCU-CPR)4a,4b and their characterizations were further investigated by IR,NMR,XRD,ROESY,TG,DSC and fluorescence spectrophotometer.Besides,by agarose gel electrophoresis,particle size and zeta potential,atomic force microscopy images to study DNA condensation.