Synthesis and immunomodulatory activity of [60]fullerene¨Ctuftsin conjugates

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• 作者：Yingying  ; Xu^a ; Jiadan  ; Zhu^a ; Kun  ; Xiang^a ; Yuankai  ; Li^a ; Ronghua  ; Sun^a ; Jie  ; Ma^b ; Hongfang  ; Sun^a ;   ; ^{shf@pku.edu.cn} ; Yuanfang  ; Liu^a ;   ; ^c ;   ; ^{yliu@pku.edu.cn}
• 关键词：Fullerene C₆₀ ; Tuftsin ; Peritoneal macrophages ; Phagocytosis ; Chemotaxis ; MHC II
• 刊名：Biomaterials
• 出版年：2011
• 出版时间：December 2011
• 年：2011
• 卷：32
• 期：36
• 页码：9940-9949
• 全文大小：1009 K

文摘

Immunomodulating peptide tuftsin (Thr-Lys-Pro-Arg) was covalently conjugated to fullerene C₆₀ by two different ways to prepare NH₂¨Ctuftsin¨CC₆₀ and C₆₀¨Ctuftsin¨CCOOH. The two new compounds were intensively characterized. The synthetic C₆₀¨Ctuftsin conjugates were assayed for their stability against leucine aminopeptidase degradation. And the immunostimulating activities to murine peritoneal macrophages were investigated in?vitro. Compared with the natural tuftsin, significant enhancement of phagocytosis, chemotaxis activities and major histocompatibility complex class II (MHC II) molecule expression were observed in macrophages stimulated by both of the conjugates. The two conjugates also exhibit complete resistance to enzymatic hydrolysis, and they are non-toxic to macrophages in the tested concentrations. On all accounts, these results suggest that the C₆₀¨Ctuftsin conjugates can be used as potential candidates of immunomodulators and vaccine adjuvants.