基于DSPE-PEG-TCO的新型反式环辛烯脂质体的构建及其反应性研究-UDP糖丨MOF丨金属有机框架丨聚集诱导发光丨荧光标记推荐西安齐岳生物

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基于DSPE-PEG-TCO的新型反式环辛烯脂质体的构建及其反应性研究

发布时间：2025-07-09 作者：zyl 分享到：

文献：BioMed Research International

文献链接：https://onlinelibrary.wiley.com/doi/full/10.1155/2014/129458

摘要：

A new lipid containing trans-cyclooctene was prepared using DSPE-PEG2000-amine and TCO-NHS ligand [52]. The liposomes contained DSPC/cholesterol/DSPE-PEG2000/DSPE-PEG2000-TCO (65/30/2.5/2.5) labeled with [18F]fluoro-1,2-dipalmitoyl glycerol and were prepared by sonication and extrusion to obtain a size distribution around 143 nm. The cyclooctene moiety was found to retain reactivity after liposome formation. In order to visualize tumor tissues with the radiolabeled liposomes using IEDDA chemistry in mice, the tetrazine ring must first be incorporated in the tumor tissue. A linear peptide (pHLIP) was conjugated to the tetrazine ring by maleimide-thiol reaction between a maleimide-tetrazine derivative and the cysteine terminated pHLIP peptide and then injected into the tumor tissue of the mice.

DSPE-PEG-TCO

使用DSPE-PEG2000-胺和TCO-NHS配体制备了一种新的含脂质的反式环辛烯。

脂质体含有用[18F]氟-1,2-二棕榈酰甘油标记的DSPC/胆固醇/DSPE-PEG2000/DSPE-PEG2000-TCO（65/30/2.5/2.5），通过超声处理和挤出制备，得到约143μm的粒径分布 nm.发现环辛烯部分在脂质体形成后保持反应性。为了使用IEDDA化学在小鼠体内用放射性标记的脂质体观察肿瘤组织，必须首先将四嗪环掺入肿瘤组织。

通过马来酰亚胺四嗪衍生物与半胱氨酸封端的pHLIP肽之间的马来酰亚胺-硫醇反应，将线性肽（pHLIP）偶联到四嗪环上，然后注射到小鼠的肿瘤组织中。