甘露糖基化对金刚烷-1-基三肽免疫刺激活性的影响。

Influence of mannosylation on immunostimulating activity of adamant-1-yl tripeptide.

机构信息

Department of Chemistry, Faculty of Science, University of Zagreb, Zagreb.

出版信息

Chem Biodivers. 2012 Jul;9(7):1373-81. doi: 10.1002/cbdv.201200008.

DOI:10.1002/cbdv.201200008

Abstract

The mannosylated derivative of adamant-1-yl tripeptide (D-(Ad-1-yl)Gly-L-Ala-D-isoGln) was prepared to study the effects of mannosylation on adjuvant (immunostimulating) activity. Mannosylated adamant-1-yl tripeptide (Man-OCH(2) CH(Me)CO-D-(Ad-1-yl)Gly-L-Ala-D-isoGln) is a non-pyrogenic, H(2) O-soluble, and non-toxic compound. Adjuvant activity of mannosylated adamantyl tripeptide was tested in the mouse model with ovalbumin as an antigen and in comparison to the parent tripeptide and peptidoglycan monomer (PGM, β-D-GlcNAc-(1→4)-D-MurNAc-L-Ala-D-isoGln-mesoDAP(εNH(2) )-D-Ala-D-Ala), a well-known effective adjuvant. The mannosylation of adamantyl tripeptide caused the amplification of its immunostimulating activity in such a way that it was comparable to that of PGM.

摘要

金刚烷-1-基三肽的甘露糖衍生物（D-(Ad-1-yl)Gly-L-Ala-D-isoGln）被制备来研究甘露糖化对佐剂（免疫刺激）活性的影响。甘露糖基化金刚烷-1-基三肽（Man-OCH(2) CH(Me)CO-D-(Ad-1-yl)Gly-L-Ala-D-isoGln）是一种非致热、水可溶和无毒的化合物。在以卵清蛋白为抗原的小鼠模型中，以及与母体三肽和肽聚糖单体（PGM，β-D-GlcNAc-(1→4)-D-MurNAc-L-Ala-D-isoGln-mesoDAP(εNH(2) )-D-Ala-D-Ala）的比较中，测试了甘露糖基化金刚烷基三肽的佐剂活性，PGM 是一种已知有效的佐剂。甘露糖基化金刚烷三肽引起其免疫刺激活性的放大，其方式与 PGM 相当。