期刊文章详细信息
Synthesis of two multivalent lactosides with anti-adhesive activity and their fluorescein-labeled and biotin-labeled derivatives
两种抗粘附活性乳糖苷及其荧光和生物素标记物的合成(英文)
文献类型:期刊文章
机构地区:[1]北京大学医学部天然药物及仿生药物国家重点实验室药学院化学生物学系,北京100191 [2]南京师范大学江苏省分子与药物生物技术学重点实验室生命科学院,江苏南京210046
出 处:《Journal of Chinese Pharmaceutical Sciences》
基 金:National Natural Science Foundation of China (Grant No 90713004);Ministry of Science and Technology of China(Grant No.2009ZX09103044.2009ZX09301-010)
年 份:2011
卷 号:20
期 号:4
起止页码:325-334
语 种:中文
收录情况:CAB、CAS、DOAJ、EMBASE、IC、JST、SCOPUS、ZGKJHX、普通刊
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.
关 键 词:ANTI-ADHESION BIOTIN FLUORESCEIN Multivalent-lactosides Synthesis
分 类 号:R914]
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