论文部分内容阅读
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。
Adherence of leukocytes to endothelial cells plays an important role in inflammation-related diseases. Previous studies showed that multivalent lactoside can inhibit this process and exert anti-inflammatory activity. We used 2-amino-1, 3-propanediol, glutamic acid as the connecting arm, the use of convergence method synthesis of bivalent lactose An-2 and tetravalent lactose Gu-4, these two compounds showed good anti-stick With activity, severe burn burn rats have good therapeutic effect. Anti-adhesion mechanism studies using the fluorescent markers Yan-2 and YGu-4 of An-2 and Gu-4 show that the target of multivalent lactoside is the integrin CD11b on leukocytes. This article reports the synthesis of these two new multivalent lactosides and their fluorescent and biotin labels.