中文摘要：

白细胞与内皮细胞的粘附在炎症相关的疾病中起着重要作用,前期研究发现的多价乳糖苷可以很好地抑制该过程而发挥抗炎活性。我们以2-氨基-1,3-丙二醇、谷氨酸为连接臂,采用收敛法合成了二价乳糖苷An-2及四价乳糖苷Gu-4,这两个化合物显示了良好的抗粘附活性,对重症烧伤休克大鼠具有较好的治疗效果。利用An-2及Gu-4的荧光标记物Yan-2和YGu-4进行的抗粘附机制研究表明,多价乳糖苷的作用靶点是白细胞上的整合素CD11b。本文将报道这两种新的多价乳糖苷及其荧光和生物素标记物的合成。

英文摘要：

Adhesion of leukocytes to endothelium plays an important role in inflammation-associated diseases.Our previous studies showed that multivalent lactosides were able to inhibit this process.Using 2-azide-l,3-propandiol and glutamic acid as spacers,we synthesized divalent lactoside An-2 and tetravalent lactoside Gu-4 by means of convergent method.These two compounds displayed high anti-adhesive activity and showed therapeutic effect in rats with severe burn shock.In addition, investigation of the anti-adhesion biological mechanism using labeled compounds YAn-2 and YGu-4 demonstrated that the target of multivalent lactosides was CD11b,theβ2 integrin subunit,on the surface of leukocytes.In this paper,the synthesis of these two new multivalent lactosides as well as their fluorescein-labeled and biotin-labeled compounds is reported.