Synthesis And The Anti-fatigue Properties Of Cyclodextrin Derivatives Based On The Supramolecular Complexation With Resveratrol Or Albumin

Supramolecular drug is the new formation of drug with high biocompatibility, low cost, low toxicity, and many other advantages. Cyclodextrin and its derivatives, as the host molecule, have been generally used as an excipient in pharmaceutics for improving certain properties of drugs, such as absorption, bioavailability, solubility and stability, by forming inclusion complexes.This thesis is divided into three chaptersthis and introduces several kinds of synthesis of cyclodextrin derivatives respectively, the interaction among cyclodextrin derivatives and resveratrol, albumin supramolecular system, and study about the inclusion of resveratrol-cyclodextrin resist sports fatigue. Specific as follows:1. The preliminary research on the synthesis and properties of cyclodextrin derivatives(1) Using ?-CD as the main body molecular, in alkaline conditions, reacting with propylene oxide and sodium chloroacetate to prepare HP-?-CD(degree of substitution: 2.431, 3.257, 2.431) and CM-?-CD(degree of substitution: 0.512, 0.814, 0.512) with different average degree of substitution;(2) study the interaction between the three cyclodextrin derivatives and bovine serum albumin, and its stability by fluorescence method.2. the interaction of Cyclodextrin derivatives with resveratrol and albumin(1) Research the inclusion compounds effect of ?-CD derivatives and resveratrol by the UV method. Experimental investigation shows that ?-CD, HP-?-CD, CM-?-CD with resveratrol can form inclusion compounds on different inclusion ratio(1:1, 1:2, 1:1). The solubility of the resveratrol were markedly improved, the solubilization multiples are 23, 39 and 21 respectively.(2) Research the inclusion form of ?-CD derivatives and resveratrol by the nuclear magnetic titration method. The experimental results show that the inclusion way of resveratrol with ?-CD is similar to resveratrol with CM-?-CD: the bis-hydroxyphenyl ring of resveratrol inserted into the cavity from small port of ?-CD and CM-?-CD.(3) Research the interaction of resveratrol, resveratrol-cyclodextrin complex and bovine serum albumin by fluorescence method. Experimental investigation shows that resveratrol and resveratrol-cyclodextrin complex has a fluorescence quenching effect on bovine serum albumin, which the resveratrol quenching effect is remarkable(?F=1079.5), using hydrophobic forces(?H > 0,?S > 0) spontaneously by non-radiative energy transfer mechanism(r < 7 nm).(3) The fatigue research of cyclodextrin derivative and the inclusion compound of resveratrol.Mice were trained to swim for the sports model, take swimming time, blood lactate and glucose, glycogen, muscle glycogen, blood urea nitrogen, aspartate aminotransferase, alanine aminotransferase, uric acid as an indicator to study white Resveratrol-cyclodextrin inclusion swimming training endurance and energy Metabolism. The experimental studies have shown that endurance training group compared with resveratrol, resveratrol-cyclodextrin inclusion can prolong swimming time, reduce blood urea nitrogen, aspartate aminotransferase, alanine aminotransferase, uric acid, increased liver glycogen, muscle glycogen content. From the point of view of energy metabolism showed the clathrate have a better effect on exercise endurance and resistance movement fatigue than resveratrol monomer, wherein the resveratrol –hydroxypropyl-?-cyclodextrin inclusion was the best one.