Study On The Polyamine-?-cyclodextrin/Morin Inclusion Complex And The Preparation Of Acyclic Cucurbiturils And The Properties Of Its Inclusion Complex

Cyclodextrin and its derivatives are widely used in drug carriers because of their good biocompatibility and hydrophobic cavity.Cyclodextrin has a special structure,the hydrophilic outer surface,hydrophobic inner cavity,which allows cyclodextrins to form inclusion compounds with poorly soluble drugs and improve the water solubility and bioavailability of poorly soluble drugs.Acyclic cucurbiturils was developed from cucurbituril and is a research hotspot in recent years.This compound contain hydrophobic flexible cavities.it's water solubility is superior than cyclodextrin or cucurbituril.And there are more possibilities for modification in structure,so it is widely used.The research content of this paper is mainly divided into the following three parts:1.Inclusion compounds of four amine-modified cyclodextrins with morin.The four inclusion compounds were characterized by one-dimensional and two-dimensional nuclear magnetic resonance hydrogen spectroscopy,ultraviolet phase solubility,X-ray powder diffraction,and scanning electron microscopy to determine them.The apparent equilibrium constant Ks and its inclusion mode are inferred to be 1:1.The results show that after the inclusion of four amino cyclodextrins,the water solubility of morin is greatly improved.The DPPH scavenging assay showed that the antioxidant activity of the morin/amino cyclodextrin inclusion complexes were improved.2.The synthetic acyclic cucurbituril M1,M2,M3 with a fluorescent group was used as a fluorescent probe to detect nicotine molecules.The experimental results show that nicotine can be very stable in buffered solution with p H 3 and quenched the fluorescence of three acyclic cucurbituril.Under the best experimental conditions,the relationship between the fluorescence quenching and concentration of nicotine and M1,M2,M3 were studied respectively,and a quantitative analysis and detection method of nicotine fluorescence was preliminarily established.3.In order to complement and improve the previous work,in this thesis,we prepared an acid-sensitive acyclic cucurbituril ACB-1,The binding constants Ks of ACB-1/camptothecin and water solubility were determined by a series of characterization and water solubility experiment.MTT method was used to measure the anticancer activity and cytotoxicity of inclusion complexes.The results showed that the water solubility of camptothecin increased greatly after the formation of inclusion compound.Although the antitumor effect of inclusion compounds were not as obvious as the monomer,the toxicity to normal cells decreased.Through the study of the model drug rhodamine dye,it was confirmed that the acid-sensitive acyclic cucurbituril can release the model drug molecules in the cavity under the weakly acidic conditions on the surface of tumor cells.