Syriltes and Biologlacal Enaluativns of Fulkren-Glycosidet.

本课题设计并开发了一种新型的糖缀合物，即“富勒烯糖缀合物”。C60缀合物由具有生物活性的活性糖苷通过n -糖苷键引入表面组成。这两种分子在物理化学和生物学方面的不同性质有望诱导出一类新的生物活性化合物。在合成“tullerene糖缀合物”之前，开发了一种高效的糖基化方法，该方法涉及使用新的硫代糖基供体和半乳糖基转移酶。新的硫代糖基供体可方便地用于形成具有高生物潜力的球状和生物苷，以捕获志贺毒素并使其失活。牛半乳糖转移酶被发现能催化一类新的酶反应，适用于非天然l糖和无环底物。几种具有生物活性的糖类通过糖酰肼与C60之间的热偶联与C60富勒烯偶联。衍生的富勒烯糖缀合物和富勒烯醇缀合物是水混溶的，并被证明具有很高的生物潜力，可以阻断碳水化合物与蛋白质的结合，参与许多生物现象。

In this research project, a new type of glycoconjugates, namely, "fullerene g ycoconjugates ' was designed and developed. The C60 conjugates are composed of biologically active active giycosides introduced onto the surface via an N-glycoside linkage. The different property of the two molecules regarding from both physicchemical and biological aspects is expected to induce a novel class of biologically active compounds.Prior to the synthesis of the'Tullerene glycoconjugates", an efficient glycosylation method was deveioped, which involved the use of new thio-glycosyl donors and galactosyltransferase. The new thio-glycosyl donor was applied conveniently to the formation of globotn- and biosides possessing high biological potential to trap Shiga toxins and deactivate the toxins. A bovine galactosyltransferase was found to catalyse a novel class of enzymic reactions applicable to non-natural L-sugars and acyclic substrates.Several types of biologiclaly active saccharides were coupled with C60 fullerene via thermal couplmg between a glycoylazide and C60. The derived fullerene glycococonjugates as well as fullerenol conjugates were water-miscible and proved to show high biological potential to block carbohydrate-protein binding involved in many biological phenomena.