文献：线粒体、溶酶体和内质网：哪个是光疗的最佳靶点？

链接：https://www.sciencedirect.com/science/article/abs/pii/S0168365922006320

作者：李艳红 ，贾浩然 ，王洪 银，华先武 ，鲍彦文 ，吴福 根

节选：

DSPE-PEG-Ce6、甲氧基（OMe）-PEG 5000 -Ce6（OMe-PEG-Ce6）和DSPE-PEG 5000-异硫氰酸荧光素（FITC）（DSPE-PEG-FITC）的合成

合成DSPE-PEG-Ce6：将1.60 mg Ce6溶于1 mL二甲基亚砜（DMSO）中。然后，将4.16 mg 1-乙基-3-（3-二甲基氨基丙基）碳二亚胺（EDC）和3.09 mg  N-羟基琥珀酰亚胺（NHS）加入上述Ce6溶液中，室温反应4 h。接着，将活化后的Ce6加入5.17 mg DSPE-PEG 5000 -NH 2（预溶于DMSO）中，继续搅拌反应过夜。将混合物用DMSO透析（截留分子量（MWCO）= 2 kDa）

DSPE-PEG-Ce6胶束的合成与表征

本设计采用DSPE-PEG 5000 -NH 2作为药物载体，因为较长的PEG链可以作为阻隔生物成分的保护屏障，从而延长药物的循环时间[30,31]。Ce6是第二代多聚苯乙烯，可通过其羧基轻松修饰进行化学结合。本设计通过EDC/NHS偶联法实现了Ce6与DSPE-PEG 5000 -NH 2的共价结合。我们利用傅里叶变换红外(FTIR)光谱法，

结论

综上所述，我们成功构建了用于成像引导和时空控制的光动力* (PDT) 的 DSPE-PEG-Ce6 胶束。我们意外地发现，DSPE-PEG-Ce6 在细胞摄取后，以时间依赖性的方式依次与线粒体、溶酶体和内质网共定位。得益于 DSPE-PEG-Ce6 的动态亚细胞分布和可调节的结合量，我们能够仔细而准确地评估位于线粒体、溶酶体和内质网的含 PS 纳米剂的光动力* (PDT) 疗效。

Section snippets

Synthesis of DSPE-PEG-Ce6, methoxyl (OMe)-PEG5000-Ce6 (OMe-PEG-Ce6), and DSPE-PEG5000-fluorescein isothiocyanate (FITC) (DSPE-PEG-FITC)

To synthesize DSPE-PEG-Ce6, 1.60 mg Ce6 was dissolved in 1 mL dimethyl sulfoxide (DMSO). Then, 4.16 mg 1-ethyl-3-(3-(dimethyl-amino)propyl)carbodimide (EDC) and 3.09 mg N-hydroxysuccinimide (NHS) were further added into the above Ce6 solution for reaction at room temperature for 4 h. Next, the activated Ce6 was added to 5.17 mg DSPE-PEG5000-NH2 (predissolved in DMSO) for further reaction under stirring overnight. The mixture was dialyzed (molecular weight cut-off (MWCO) = 2 kDa) against DMSO

Synthesis and characterization of DSPE-PEG-Ce6 micelles

DSPE-PEG5000-NH2 was adopted as a drug carrier in our design because the long PEG chain can serve as a protective barrier against the biological components to prolong the circulation time of the encapsulated drug [30,31]. Ce6 is a second-generation PS and can be easily modified through its carboxyl groups for chemical conjugation. In our case, covalent binding of Ce6 to DSPE-PEG5000-NH2 was realized through the EDC/NHS coupling method. We used Fourier transform infrared (FTIR) spectroscopy,

Conclusions

In summary, we successfully fabricated DSPE-PEG-Ce6 micelles for imaging-guided and spatiotemporally-controlled PDT. We surprisingly found that DSPE-PEG-Ce6 colocalized with mitochondrion, lysosome, and ER successively after cellular uptake in a time-dependent manner. Benefiting from the dynamic subcellular distribution of DSPE-PEG-Ce6 with tunable binding amounts, we were able to carefully and accurately evaluate the PDT efficacies of the PS-containing nanoagents located at the mitochondrion,

西安齐岳生物提供相关产品：

YIGSR-PEG-DSPE

APRPG-PEG-DSPE

NGR-PEG-DSPE

NGR(c(GGCNGRC))-PEG-DSPE

RVG29-PEG-DSPE

THRPPMWSPVWP-PEG-DSPE

M2pep-PEG-DSPE

EB1-PEG-DSPE

CPP-PEG-DSPE

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