Synthesis And Study Of Scutellarin-Cyclodextrin Conjugate And Polyrotaxane

Drug cyclodextrin conjugate and drug cyclodextrin conjugate polyrotaxane have been the significant topic of supramolecular chemistry and material chemistry. In order to study the routes of synthsis cyclodextrin conjugate, we choose-d butyric and scutellarin which have some anti-inflammatory activity and some anticancer activity. We have confirmed the structure of the conjugate and the polyrotaxane. We also reseach the nature of the conjugate and the polyrotaxane. The cytotoxicity tests for the conjugate and the polyrotaxane have been evaluated in vitro for antiproliferative activity by the MTT cytotoxicity assay. In this paper, we use cyclodextrin derivatives to prepare a novel polyrotaxane with a high solubility. The major contents of this thesis are as follows:1. We have modified the cyclodextrin and prepare6-O-succinyl-β-CD、6-O-N3-β-CD、6-OTs-a-CD、6-OTs-β-CD,6-OTs-γ-CD。We confirm the structure by1H NMR. I prepare the raw materials for the follow-up experiments.2. I have synthsised6-O-butiric-(3-CD conjugate by use CDI and butyric sodium. I confirm the structure by1H NMR and compare the two routes. Prepare6-O-SCU-α-,-β-,-γ-CD, confirm the structure by1H NMR,13C NMR, high resolution mass. Use DSC, X-RAY diffraction to observe the physical nature. The cytotoxicity tests for the conjugate and the polyrotaxane have been evaluated in vitro for antiproliferative activity by the MTT cytotoxicity assay.3.We prepare pseudorotaxane by use PPG and N3CD then use6-O-succinyl-β-CD as stoppers. Transform the azido to amino, we get amino cyclodextrin polyrotaxane. Then we use scutellarin to reation with the polyrotaxane, we get scu-polyrotaxane conjugate. We confirm the structure of the polyrotaxane by1H NMR. Use DSC, X-RAY diffraction to observe the physical nature. We study the process of fracture of polyrotaxane by the assay of fluorescence intensity. The cytotoxicity tests for the conjugate and the polyrotaxane have been evaluated in vitro for antiproliferative activity by the MTT cytotoxicity assay.