Syriltes and Biologlacal Enaluativns of Fulkren-Glycosidet.

在这个研究项目中，设计和开发了一种新型的糖缀合物，即“富勒烯糖缀合物”。C60缀合物由通过N-糖苷键引入表面的具有生物活性的活性糖苷组成。两种分子在物理化学和生物学方面的不同性质预计会诱导出一类新型的生物活性化合物。在合成“富勒烯糖缀合物”之前，开发了一种有效的糖基化方法，其中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应用于形成球蛋白和生物苷，它们具有捕获志贺毒素并使毒素失活的高生物潜力。牛半乳糖基转移酶被发现可催化一类适用于非天然 L-糖和无环底物的新型酶反应。几种类型的生物活性糖通过乙酰叠氮化物和 C60 之间的热耦合与 C60 富勒烯偶联。衍生的富勒烯糖缀合物以及富勒烯醇缀合物可与水混溶，并被证明显示出阻断许多生物现象中涉及的碳水化合物-蛋白质结合的高生物潜力。

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.